- Synthesis of methanesulfonyl chloride (MSC) from methane and sulfuryl chloride
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Methane is transformed selectively to methanesulfonyl chloride at low temperature by liquid-phase reaction of methane with SO2Cl 2 in the presence of a free radical initiator and a promoter using 100% H2SO4 as the solvent.
- Mukhopadhyay, Sudip,Zerella, Mark,Bell, Alexis T.,Srinivas, R. Vijay,Smith, Gary S.
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- Experimental study on deep desulfurization of MTBE by electrochemical oxidation and distillation
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With the increasing awareness of environmental protection, deep desulfurization of methyl tert-butyl ether (MTBE), which is the most important octane booster in gasoline, is extremely urgent. Herein, a new desulfurization method, involving the combination of electrochemical oxidation and distillation, is proposed to reduce the sulfur content in MTBE. Under optimum operating conditions, the sulfur content of real MTBE decreases from 132.5 μg g-1 to 2.3 μg g-1 and the desulfurization efficiency reaches 98.25%. The oxidation products with high boiling points can be separated by distillation. FTIR analyses prove that electrochemical oxidation has no influence on the main properties of MTBE. Moreover, GC/MS is used to study the conversion of model organic sulfides (dimethyl disulfide, diethyl sulfide and butyl mercaptan) in the electrochemical oxidative desulfurization process. Finally, the possible reaction mechanism of the electrochemical oxidative desulfurization of MTBE is proposed.
- Li, Jing-Jing,Zhou, Fei,Tang, Xiao-Dong,Hu, Tao,Cheng, Jin
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- Novel One-Step Synthesis of Sulfonyl Chlorides from Sulfides with Iodosobenzene and Hydrogen Chloride-Treated Silica Gel
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Alkyl and aryl benzyl sulfides were conveniently converted into the corresponding alkyl and aryl sulfonyl chlorides in high yields with a few minutes' pulverization of solid mixtures with iodosobenzene and hydrogen chloride-treated silica gel.
- Sohmiya, Hajime,Kimura, Takahide,Fujita, Mitsue,Ando, Takashi
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- A practical and efficient method for the preparation of sulfonamides utilizing Cl3CCN/PPh3
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Cl3CCN in combination with PPh3 proved to be a highly reactive reagent for the conversion of sulfonic acids to the corresponding sulfonyl chlorides in refluxing CH2Cl2. Upon reaction with amines, the corresponding sulfonamides were obtained in good to excellent yields.
- Chantarasriwong, Oraphin,Jang, Doo Ok,Chavasiri, Warinthorn
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- Novel anti-cancer agents based on germacrone: design, synthesis, biological activity, docking studies and MD simulations
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Germacrone is a major activity component found in Curcuma zedoaria oil product, which is extracted from Curcuma zedoaria. In the present study, novel germacrone derivatives were first designed based on the theories of bioalkylating agents, synthesized, and then investigated for their inhibition effects on Bel-7402, HepG2, A549, and HeLa cells. Moreover, the study also evaluated the inhibition of these derivatives on c-Met kinase, which is expressed in a number of cancers. The results indicated that most of the compounds showed a stronger inhibitory effect on cancer cells and c-Met kinase than germacrone. Besides these findings, molecular docking studies were also carried out to analyze the results and explain the molecular mechanism of activities to c-Met kinase. Molecular dynamics simulations have been carried out for the further evaluation of binding stabilities between the compounds and their receptors.
- Ye, Lianbao,Wu, Jie,Chen, Weiqiang,Feng, Yu,Shen, Zhibing
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- FTIR Kinetic and Mechanistic Study of the Atmospheric Chemistry of Methyl Thiolformate
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Some aspects of the atmospheric chemistry of methyl thiolformate (CH3SCHO), a recently detected intermediate in the oxidation of dimethyl sulfide, have been investigated at 298 K and 1000 mbar total pressure in large reaction chambers using long path in situ FTIR absorption spectroscopy for the analysis.Rate coefficients of (1.11 +/- 0.22)E-11 and (5.80 +/- 0.80)E-11 cm3 molecule-1 s-1 have been determined for its reaction with OH radicals and Cl atoms, respectively.The UV spectrum of CH3SCHO has been measured in the range 220-355 nm and a lower limit of 5.4 days determined for its atmospheric photolytic lifetime.Detailed product analyses have made for the OH and Cl initiated photooxidation of CH3SCHO.Strong SO absorption bands observed in both systems are tentatively assigned to CH3SOCHO in the OH system and to CH3SOCl in the Cl system.The first gas-phase spectra of CH3SCl and CH3SOCl are also presented.The results are discussed with respect to the atmospheric chemistry of CH3SCHO and possible consequences for the photooxidation mechanism of dimethyl sulfide.
- Patroescu, Iulia V.,Barnes, Ian,Becker, Karl H.
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Read Online
- METHOD FOR PRODUCING TRIAZOLE COMPOUND
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A compound represented by formula (5)can be produced by simultaneously and separately adding a compound represented by formula (4)and methanesulfonyl chloride to a compound represented by formula (3)and a compound represented by formula (6)having excellent control efficacies against pests can be produced by subjecting the compound represented by formula (5) to intramolecular condensation in the presence of an acid.
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- Selective Late-Stage Sulfonyl Chloride Formation from Sulfonamides Enabled by Pyry-BF4
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Reported here is a simple and practical functionalization of primary sulfonamides, by means of a pyrylium salt (Pyry-BF4), with nucleophiles. This simple reagent activates the poorly nucleophilic NH2 group in a sulfonamide, enabling the formation of one of the best electrophiles in organic synthesis: a sulfonyl chloride. Because of the variety of primary sulfonamides in pharmaceutical contexts, special attention has been focused on the direct conversion of densely functionalized primary sulfonamides by a late-stage formation of the corresponding sulfonyl chloride. A variety of nucleophiles could be engaged in this transformation, thus permitting the synthesis of complex sulfonamides, sulfonates, sulfides, sulfonyl fluorides, and sulfonic acids. The mild reaction conditions and the high selectivity of Pyry-BF4 towards NH2 groups permit the formation of sulfonyl chlorides in a late-stage fashion, tolerating a preponderance of sensitive functionalities.
- Gómez-Palomino, Alejandro,Cornella, Josep
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supporting information
p. 18235 - 18239
(2019/11/13)
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- METHOD OF CONVERTING ALKANES TO ALCOHOLS, OLEFINS AND AROMATICS
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A cost-effective and energy-efficient process is disclosed for converting a methane-containing gas to a methane sulfonyl halide comprising reacting the methane-containing gas, under illumination by a light emitting diode (LED) source, with a sulfuryl halide or a halogen in the presence of sulfur dioxide, whereby the methane sulfonyl halide is obtained for isolation or further reactions. The further reactions may sequentially include, in order, contacting the methane sulfonyl halide with a catalyst complex to form a methane monohalide; catalytically converting the methane monohalide to a value-added chemical such as an alcohol, an olefin, an aromatic, derivatives thereof, or mixtures thereof; releasing any hydrogen halide formed in the process; and converting the hydrogen halide to a halogen and recycling it for re-use.
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Paragraph 0052-0053
(2019/08/08)
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- BIODEGRADABLE POLYETHYLENE GLYCOL DERIVATIVE HAVING CYCLIC BENZYLIDENE ACETAL LINKER
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A biodegradable polyethylene glycol derivative in which a polyethylene glycol chain is linked by an acetal linker capable of accurately controlling the hydrolysis rate under different pH environments in the living body, and whose division rate into a polyethylene glycol chain of low molecular weight in the living body can be accurately controlled. The biodegradable polyethylene glycol derivative is represented by formula (1) or formula (2) as described.
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- A α-pinene derivatives and its preparation method and application (by machine translation)
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This invention has offered a kind of α-pinene derivatives, the derivatives of formula I such as a structural formula shown in formula II. Said α-pinene derivatives by the reduction, the organic acid ester and the like introduced into the α-pinene in the molecule skeleton to obtain new derivatives. Research shows that in vitro anti-tumor activity, the present invention provides the α-pinene derivatives to liver cancer cells has significant inhibition function, as the preparation of anti-tumor compound or its pharmaceutically acceptable salt, hydrate, solvate or prodrug, has good application prospect. Type I ;? ? ? Type II. (by machine translation)
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Paragraph 0168; 0169
(2016/10/09)
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- A recycled by-product hydrochloric acid method of preparing methyl sulfonic acid
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The invention relates to a method for preparing methanesulfonic acid by recycling a byproduct, namely hydrochloric acid. The method is characterized in that a method of hydrogen chloride, chlorine gas, methanesulfonic acid and hydrogen chloride is adopted, and the byproduct, namely the hydrochloric acid is recycled in the preparation process of the methanesulfonic acid to prepare the methanesulfonic acid. The method has the advantages that the byproduct, namely the hydrochloric acid is adopted for preparing chlorine gas and directly reacted with dimethyl disulfide, so that the safety risk and the logistics cost in purchase, transportation and storage of the chlorine gas with severe toxicity can be avoided; the byproduct, namely the hydrochloric acid, which is difficult to sell can be locally digested and utilized, and turned into treasure, so that the byproduct, namely the hydrochloric acid becomes a main raw material for preparing the methanesulfonic acid and the recycling of chlorine element is realized. Simultaneously, leftover manganese dioxide waste after oxidation reaction of potassium permanganate is utilized to prepare manganese chloride, and the manganese chloride can be used for electrolytic manganese, so that the production cost and the safety risk of the methanesulfonic acid are greatly reduced, and two major restricting factors, namely the chlorine gas and the byproduct, namely the hydrochloric acid in the preparation method of the methanesulfonic acid are simultaneously eliminated.
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Paragraph 0054; 0055; 0056; 0057; 0058; 0059
(2016/10/07)
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- HIV INTEGRASE INHIBITORS
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The present invention features compounds that are HIV integrase inhibitors and therefore are useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.
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- Tert -Butyl Hypochlorite Mediated Oxidative Chlorination of S -Alkylisothiourea Salts: Synthesis of Sulfonyl Chlorides
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Under neutral conditions, a variety of S-alkylisothiourea salts were smoothly converted into the corresponding sulfonyl chlorides through tert-butyl chlorite mediated oxidative chlorination in good to excellent yields after simple purification. In addition to the environmental and procedural advantages of this method, the neutral conditions potentially make it applicable to substrates that bear acid-sensitive functional groups. For example, the Cbz-protected 2-aminoethanesulfonyl chloride could be synthesized in moderate to good yields under the current neutral conditions, and the acid-sensitive Cbz-protecting group was not affected.
- Qiu, Kui,Wang, Rennan
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p. 3186 - 3190
(2015/10/19)
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- Clean and economic synthesis of alkanesulfonyl chlorides from S-alkyl isothiourea salts via bleach oxidative chlorosulfonation
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A simple procedure for clean and economic synthesis of alkanesulfonyl chlorides via bleach-mediated oxidative chlorosulfonation of S-alkyl isothiourea salts is disclosed. This procedure is environment- and worker-friendly with the advantages of readily accessible materials and reagents, simple and safe operations, easy purification without chromatography, and affords high yields of up to 99%.
- Yang, Zhanhui,Zhou, Bingnan,Xu, Jiaxi
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p. 225 - 229
(2014/03/21)
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- Convenient and environment-friendly synthesis of sulfonyl chlorides from S -alkylisothiourea salts via N-chlorosuccinimide chlorosulfonation
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A convenient, practical, and environmentally friendly method for the synthesis of sulfonyl chlorides has been developed. Structurally diverse sulfonyl chlorides were synthesized in moderate to excellent yields from S-alkylisothiourea salts, which can be easily prepared from readily accessible alkyl halides or mesylates and inexpensive thiourea, via N-chlorosuccinimide chlorosulfonation. In large-scale syntheses, the byproduct succinimide from 'waste water' can be conveniently converted into the starting reagent N-chlorosuccinimide with sodium hypochlorite (bleach) to make the method sustainable. Georg Thieme Verlag Stuttgart, New York.
- Yang, Zhanhui,Xu, Jiaxi
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p. 1675 - 1682
(2013/07/27)
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- IMPROVED PROCESS FOR THE SULFOCHLORINATION OF HYDROCARBONS
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Produce a sulfo-chlorinated hydrocarbon using liquid sulfur dioxide, a chlorinating agent such as chlorine or sulfuryl chloride, and a metal complex catalyst, the catalyst being represented as LnM where L is at least one of an amine, phosphine, chloride or oxide, n is an integer within a range of from 1 to 6, and M is a metal selected from a group consisting of copper (Cu), ruthenium (Ru), iron (Fe), chromium (Cr), lanthanum (La), nickel (Ni), palladium (Pd), rhodium (Rh), rhenium (Re), molybdenum (Mo) and manganese (Mn).
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Page/Page column 3-4
(2011/02/24)
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- A convenient, one-pot procedure for the preparation of acyl and sulfonyl fluorides using Cl3CCN, Ph3P, and TBAF(t -BuOH) 4
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Various carboxylic acids were converted into acyl fluorides in excellent yields by treatment with trichloroacetonitrile, triphenylphosphine, and TBAF(t-BuOH)4 at room temperature. The reaction was applicable to the preparation of acid-sensitive amino acid fluorides without deprotection or rearrangement
- Kim, Joong-Gon,Jang, Doo Ok
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experimental part
p. 3049 - 3052
(2011/02/25)
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- One-Pot synthesis of sulfonamides from primary and secondary amine derived sulfonate salts using cyanuric chloride
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A convenient, mild and efficient one-pot synthesis of new sulfonamides is described. The reaction of primary or secondary amine derived sulfonate salts in the presence of cyanuric chloride, triethylamine as base, and anhydrous acetonitrile as solvent at room temperature gives the corresponding sulfonamides in good to excellent yields. Georg Thieme Verlag Stuttgart.
- Rad, Mohammad Navid Soltani,Khalafi-Nezhad, Ali,Asrari, Zeinab,Behrouz, Somayeh,Amini, Zohreh,Behrouz, Marzieh
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experimental part
p. 3983 - 3988
(2010/03/26)
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- An easy microwave-assisted synthesis of sulfonamides directly from sulfonic acids
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(Chemical Equation Presented) An easy and handy synthesis of sulfonamides directly from sulfonic acids or its sodium salts is reported. The reaction is performed under microwave irradiation, has shown a good functional group tolerance, and is high yielding.
- De Luca, Lidia,Giacomelli, Giampaolo
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p. 3967 - 3969
(2008/09/19)
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- One-electron reduction of methanesulfonyl chloride. The fate of MeSO 2CI?- and MeSO2? intermediates in oxygenated solutions and their role in the cis-trans isomerization of mono-unsaturated fatty acids
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The one-electron reduction of methanesulfonyl chloride (MeSO2Cl) leads, in the first instance, to an electron adduct MeSO2Cl ?- which lives long enough for direct detection and decays into sulfonyl radicals MeSO2? and Cl-, with k = 1.5 × 106 s-1. Both, MeSO2Cl ?- and MeSO2? showed a similar absorption in the UV with λmax of 320 nm. In the presence of oxygen, MeSO 2Cl?- transfers an electron to O2 and establishes an equilibrium with superoxide. The rate constant for the forward reaction was measured to 4.1 × 109 M-1 s -1, while for the back reaction only an interval of 1.7 × 105 to 1.7 × 106 M-1 s-1 could be estimated, with a somewhat higher degree of confidence for the lower value. This corresponds to an equilibrium constant in the range of 2.4 × 10 3 to 2.4 × 104. With reference to E°(O 2/O2?-) = -155 mV, the redox potential of the sulfonyl chloride couple, E°(MeSO2Cl/MeSO2Cl ?-), thus results between being equal to -355 and -414 mV (vs NHE). MeSO2Cl?- reduces (besides O2) 4-nitroacetophenone. The underlying electron transfer took place with k = 1.5 × 109 M-1 s-1, corroborating an E° for the sulfonyl chloride couple significantly exceeding the above listed lower value. The MeSO2? radical added to oxygen with a rate constant of 1.1 × 109 M-1 s-1. Re-dissociation of O2 from MeSO2OO? occurred only very slowly, if at all, that is, with k ? 105 s-1. MeSO 2? radicals can act as the catalyst for the cis-trans isomerization of several Z- and E-mono-unsaturated fatty acid methyl esters in homogeneous solution. The effectiveness of the isomerization processes has been addressed, and in the presence of oxygen the isomerization is completely suppressed.
- Tamba, Maurizio,Dajka, Katalin,Ferreri, Carla,Asmus, Klaus-Dieter,Chatgilialoglu, Chryssostomos
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p. 8716 - 8723
(2008/02/13)
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- Chlorotrimethylsilane-nitrate salts as oxidants: Direct oxidative conversion of thiols and disulfides to sulfonyl chlorides
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(Chemical Equation Presented) A mixture of nitrate salt and chlorotrimethylsilane is found to be a mild and efficient reagent for the direct oxidative conversion of thiols (1) and disulfides (2) to the corresponding sulfonyl chlorides (3) in excellent yields through oxidative chlorination. Sulfides and sulfoxides were also found to undergo oxidation to sulfones under similar reaction conditions. In most cases these reactions are highly selective, simple, and clean, affording products in high yield and purity.
- Prakash, G. K. Surya,Mathew, Thomas,Panja, Chiradeep,Olah, George A.
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p. 5847 - 5850
(2008/02/09)
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- Modified bio-related substance, process for producing the same, and intermediate
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A modified bio-related substance, wherein at least one poly(alkylene glycol)oxy group represented by the following formula (1) is combined in a molecule: wherein R is a hydrocarbon group having 1 to 24 carbon atoms, OA1 and OA2 are each an oxyalkylene group having 2 to 4 carbon atoms, the groups represented by R are the same or different from each other in one molecule, and the groups represented by OA2 are the same or different from each other in one molecule, n and m are each average number of moles of the oxyalkylene group added, n represents 0 to 1000, and m represents 10 to 1000.
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- Method for photochemical sulfochlorination of gaseous alkanes
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The invention concerns a method for making an alkanesulponyl chloride by photochemical reaction of an alkane with chlorine and sulphur dioxide, which consists in using as light source an indium-doped medium-pressure mercury lamp.
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- 13-substituted milbemycin derivatives, their preparation and their use against insects and other pests
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Compounds of formula (I) and salts thereof: Wherein R1 represents methyl, ethyl, isopropyl or s-butyl; and R2 represents hydrogen or alkyl. R3 represents hydrogen, optionally substituted alkanoyl, optionally substituted alkenoyl, optionally substituted alkynoyl, alkylsulfonyl, or alkoxycarbonyl, or R2 and R3 together with the nitrogen atom to which they are attached form a saturated, optionally substituted 4- to 6-membered heterocyclic ring group. The moiety -a- together with the carbon atom to which it is attached forms a 3- to 6-membered cycloalkyl group. These compounds have anthelmintic, acaricidal and insecticidal activity.
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- Process for functionalising a phenolic compound carrying an electron-donating group
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The invention concerns a method for functionalizing a phenolic compound bearing an electron-donor group, in said group para position, inter alia a method for the amidoalkylation of a phenolic compound bearing an electron-donor group, and more particularly, a phenolic compound bearing an electron-donor group preferably, in the hydroxyl group ortho position. The method for functionalizing in para position with respect to an electron-donor group carried by a phenolic compound is characterised in that the phenolic compound bearing an electron-donor group is subjected to the following steps: a first step which consists of protecting the hydroxyl group in the form of a sulphonic ester function; a second step which consists in reacting the protected phenolic compound with an electrophilic reagent; optionally, a third step deprotecting the hydroxyl group.
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- A new, mild preparation of sulfonyl chlorides
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A new method was developed for the preparation of sulfonyl chlorides from sulfonic acids under neutral conditions using 2,4,6-trichloro-1,3,5-triazine as chlorinating agent.
- Blotny, Grzegorz
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p. 1499 - 1501
(2007/10/03)
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- Thiopyridines for use in the control of helicobacter bacteria
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PCT No. PCT/EP95/02236 Sec. 371 Date Sep. 16, 1997 Sec. 102(e) Date Sep. 16, 1997 PCT Filed Jun. 9, 1995 PCT Pub. No. WO95/34553 PCT Pub. Date Dec. 21, 1995Thiopyridines of formula (I) in which the substituents and symbols are as defined in the specification are suitable for use in controlling Helicobacter bacteria. They are compounded into medicament compositions and administered to subjects afflicted with a disease based on Helicobacter bacteria.
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- Pharmaceutical compounds
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A pharmaceutical compound of the formula: STR1 in which n is 1 or 2, R1 is --CO2 H, R2 is hydrogen or C1-4 alkyl and R3 is hydrogen, C1-10 alkyl, C2-10 alkenyl, optionally substituted phenyl, optionally substituted phenyl-C1-4 alkyl, optionally substituted phenyl C2-10 alkenyl,(optionally substituted phenyl)2 -C1-4 alkyl, optionally substituted C3-7 cycloalkyl, optionally substituted C3-7 cycloalkyl-C1-4 alkyl or optionally substituted C3-7 cycloalkyl-C2-10 alkenyl, or R2 and R3, together with the carbon atom to which they are attached, form an optionally substituted C4-7 cycloalkyl group; or a salt or ester thereof other than the compounds γ-propylidene-L-glutamic acid, γ-ethylidene-L-glutamic acid and γ-methylidene-L-glutamic acid.
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- Solid-state organic reactions proceeding by pulverization: Oxidation and halogenation with iodosobenzene and inorganic solid-supports
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Pulverization-activation method was employed to accelerate solid-state organic reactions. Crushing and grinding of solid mixtures of hydrogen halide-treated silica gels, iodosobenzene and organic substrates in the absence of a solvent brought about smooth and rapid reactions to give halogenated and/or oxidized products in good yields. Various sulfides were smoothly converted to sulfonyl chlorides in one step in excellent yields. The surface of silica gel activated by pulverization serves as a reaction field on which reagent molecules can effectively encounter with each other.
- Sohmiya, Hajime,Kimura, Takahide,Fujita, Mitsue,Ando, Takashi
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p. 13737 - 13750
(2007/10/03)
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- Process for the preparation of azine-carboxylic acid chlorides
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The invention relates to an effective and efficient process for the preparation of azinyl acid chloride compounds of formula I, wherein, Az represents an optionally substituted azinyl group, which comprises heating a trichloromethylazine of formula II Az-CCl3wherein Az has the meaning given,with an acid, that forms an acid chloride, which can be distilled off during the reaction under reduced pressure, in the presence of an acidic catalyst;, ???and to the use of the compounds of formula I obtained according to this process for the preparation of (hetero)aryloxyazinylcarboxamides of formula VI in which Az has the meaning given in any of the preceding claims, and, Ar represents an optionally substituted aryl or heteroaryl group,R3represents a hydrogen atom or an alkyl group, and, R4represents an optionally substituted alkyl, aryl, heteroaryl or cycloalkyl group.
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- HYDROXAMIC ACID AND CARBOXYLIC ACID DERIVATIVES, PROCESS FOR THEIR PREPARATION AND USE THEREOF
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This disclosure relates to a novel class of hydroxamic and carboxylic acid based matrix metalloproteinase inhibitor derivatives. The disclosure further relates to pharmaceutical compositions containing such compounds and to the use of such compounds and compositions in the treatment of matrix metalloproteinase induced diseases.
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- 1-(3'-fluoro-2',3'-dideoxy-β-D-ribofuranosyl)-5-substituted pyrimidine nucleosides
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A 2',3'-deoxy-3'-fluoro-pyrimidine nucleoside having the formula: STR1 wherein R1 is OH or NH2 ; R2 is CF3, CH2 CH2 CH3, STR2 CH2 OCH3, CH2 SCH3, CH=CH2 CH=CH--CH3, C CH, C C--CH3 or CH2 --C CH; or a pharmaceutically acceptable salt thereof. These nucleoside analogs exhibit antiviral activity against HIV.
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- Hydrazones and their use as herbicides
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wherein R1, R2, R3, R4 and R5 have those meanings as described in the specification, processes for their preparation, and the use of the new compounds as herbicides.
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- SUBSTITUTED SULPHONAMIDES, PHARMACEUTICALS THEREOF AND METHODS OF USING THEM
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The present invention concerns compounds of the formula: STR1 where R 1 is an alkyl or alkenyl radical containing up to 6 carbon atoms, a cycloalkyl radical containing 3 to 7 carbon atoms, an aralkyl, aralkenyl or aryl radical in which the aryl radical or moiety can be substituted one or more times by halogen, C 1-C 6-alkyl, C 1-C 6-alkoxy, hydroxyl, trifluoromethyl, cyano, nitro, amino, C. sub.1-C 6-alkylamino, C. sub.2-C 12-dialkylamino, C 1-C. sub.6-acylamino, C 1-C 16-acyl, C 1-C 6-alkylsulphenyl,-sulphinyl or-sulphonyl or by azido, R 2 is hydrogen atom or a C 1-C 6-alkyl, aralkyl, aralkenyl or acyl radical, A and B are saturated or unsaturated alkylene chains containing up to 10 carbon atoms which can be substituted one or more times by C. sub.1-C. sub.3-alkyl radicals, the sum of carbon atoms in chains A and B being at least 4 and at most 11, Q is an oxygen or sulphur atom, a sulphonyl or sulphinyl group or an amino group--N(R 2)--, R 2 having the same meaning as above, and Y is a free carboxylic acid group or a carboxylic acid ester, carboxylic acid amide, hydroxymethyl or tetrazolyl radical; the pharmacologically acceptable salts thereof and the optically active and E-Z isomers thereof, as well as mixtures thereof. These compounds are useful as they have an antagonistic action towards thromboxane A 2 as well as against prostaglandin endoperoxide. They inhibit the aggregation of blood platelets and prevent the constriction of the smooth musculature as well as bronchoconstriction.
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- POLYSULFONYLAMINE: TEIL XXVIII. REAKTION VON N-CHLORDIMESYLAMIN MIT EINIGEN PHSPHOR(III)-VERBINDUNGEN. ROENTGENSTRUKTURANALYSEN VON (1+)N(SO2Me)2(1-)*CH2Cl2 UND (PhO)3P=NSO2Me
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N-Chloro-dimesylamine ClN(SO2Me)2 (1) reacts with the appropriate triorganophosphines to give the ionic chloro(triorgano)phosphonium dimesylamides R3PCl(1+)*N(SO2Me)2(1-) .The reaction of 1 with (MeO)3P affords (MeO)2P(O)Cl and MeN(SO2Me)2; its reaction with (PhO)3P or PCl3 leads to elimination of MeSO2Cl and formation of the phosphine imides Y3P=NSO2Me .The (1/1) dichloromethane solvate of 2a crystallizes in the monoclinic space group P21/c with a = 1735.6(7), b = 841.1(4), c = 1658.4(7) pm, β = 118.34(3) deg, U = 2.1309(16)nm3, Z = 4.The crystal lattice consists of discrete iPr3PCl(1+) cations (P-Cl 199.4 pm, bond angles at P 105.7-117.5 deg), (MeSO2)2N(1-) anions and CH2Cl2 molecules apparently hydrogen-bonded to oxygen atoms of the anions. 3a crystallizes in the monoclinic space group P21/c with a = 974.7(3), b = 2052.3(6), c = 959.5(3) pm, β = 98.820(14) deg, U = 1.8967(10) nm3, Z = 4.The dimensions of the molecule (P-N 154.4, N-S 159.8 pm, P-N-S 126.2 deg) are consistent with a delocalized electronic structure in the P-N-S system. Key words: N-Chloro-dimesylamine; triorganophsphines; triorganophosphites; phosphorus trichloride; chloro(triorgan)phosphonium dimesylamides; N-mesyl phosphine imides; X-ray structures:
- Blaschette, A.,Jones, P. G.,Naeveke, M.,Schulte-Koerne, E.
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p. 211 - 221
(2007/10/02)
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- IMIDAZOPYRIDINES, COMPOSITIONS AND USE
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1,3-dihydro-2H-imidazo[4,5-b]pyridin-2-ones having an aryl or heteroaryl group in the 6-position, useful as phosphodiesterase inhibitors, are prepared by reacting a 2-amino-5-(aryl or heteroaryl)pyridine-3-carboxylic acid with diphenylphosphoryl azide. The compounds are of the formula where R1 and R3 are hydrogen or lower-alkyl, R5 is lower-alkyl or fluorinated lower-alkyl, and Ar is 4-or 3-pyridinyl, or N-oxides thereof, or phenyl or substituted phenyl.
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- S-Alkyl Alkanesulfonothioates and S-1-Chloroalkyl Alkanesulfonothioates from Linear Alkanesulfinyl Chlorides
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Treatment of linear alkanesulfinyl chlorides 1 with dry N,N-dimethylmethanamide (DMF), N,N-dimethylethanamide (DMA), or 1-methyl-2-pyrrolidone (NMP) in an inert atmosphere, with or without added solvent, gives S-alkyl alkanesulfonothioates 4 (minor products) and S-1-chloroalkyl alkanesulfonothioates 5.The yield of 4 is decreased in the presence of the radical inhibitor 1,4-dihydroxybenzene.Evidence has been obtained for the formation and trapping of sulfines (including methanethial S-oxide) and for formation of sulfinyl radicals, vic-disulfoxides (α-disulfoxides), and O,S-sulfenyl sulfinates as reaction intermediates.S-Phenyl benzenesulfonothioate is a major product from the reaction of alkanesulfinyl chlorides and benzenesulfinyl chloride in the presence of DMF.
- Freeman, Fillmore,Keindl, Monica C.
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p. 2026 - 2031
(2007/10/02)
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- Selectivite de la scission Si-C dans des composes du type Me3SiCH2Σ; une synthese originale et sure de l'iodoacetate d'ethyle
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The regiochemistry of the electrophilic cleavage of the SiCsp3 bond in compounds Me3SiCH2Σ (Σ = Me, Pr, Cl, COOEt) and Me3SiCHΣ2 (Σ = Cl) has been investigated using ICl, Me3SiOSO2Cl and HO3SCl as the electrophiles.When Σ = Pr or Cl a regioselective cleavage of the Si-CH3 bond was observed, producing silylated chlorosulfonates or sulfates which often were new compounds.With Σ = COOEt a regiospecific splitting of the Si-CH2COOEt bond was observed.This confirms the synthetic potential of ethyl trimethylsilylacetate.
- Bordeau, M.,Djamei, S. M.,Dunogues, J.
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p. 413 - 417
(2007/10/02)
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- Observation of Intermediates during the Reaction of Linear Alkanesulfinyl Chlorides with Activated Zerovalent Zinc
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Methane- (2), ethane- (3), propane- (4), butane (5), pentane- (6), hexane- (7), octane- (8), and dodecanesulfinyl chloride (9) reacted with activated zinc to give the corresponding alkanesulfonothioic S-alkyl esters (12-19) in 40-89percent yield.The reaction of methanesulfinyl chloride (2) with activated zerovalent zinc under nitrogen in anhydrous diethyl ether at -30, -20, and 0 deg C was investigated by 1H NMR and 13C NMR spectroscopy.The 13C NMR spectrum of the partially converted -30 deg C reaction mixture showed the presence of methanesulfinyl chloride (2), S-methyl methanesulf onothioate (12), methanesulfinic acid (24) or zinc methanesulfinate (25), methanesulfonyl chloride (26), dimethyl sulfide (27), S-methyl methanesulfinothioate (28), and methanesulfinyl methyl sulfone (29). vic-Dimethyl disulfoxides (31) and OS-methyl methanesulfino(thioperoxoates) (32) are proposed as two of several transient reaction intermediates.
- Freeman, Fillmore,Angeletakis, Christos N.,Keindl, Monica C.
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p. 454 - 458
(2007/10/02)
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- Mechanism in the chlorinolysis of sulfinyl chlorides
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The successful synthesis and chlorinolysis of α-mercaptodimethyl sulfone have provided additional support for our contention that Pummerer rearrangements may occur during the chlorinolyses of α-sulfonyl sulfinyl chlorides.Further exploration of chlorinolyses of α-sulfonyl systems has uncovered the first observation of CS bond cleavage during the chlorinolyses of (i) a sulfinyl chloride and (ii) a sulfinate ester.
- Ahern, Terence Patrick,Haley, Michael Francis,Langler, Richard Francis,Trenholm, June Ellen
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p. 610 - 614
(2007/10/02)
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- Process for the preparation of 24,24-difluoro-1α,25-dihydroxy vitamin D3 and intermediates obtained therefrom
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The present invention relates to a process and intermediates for the preparation of 24,24-difluoro-1α,25-dihydroxycholecalciferol from the readily-available 1α,3β-dihydroxyandrost-5-en-17-one which is made by a known microbiological process from 3β-hydroxyandrost-5-en-17-one [R. M. Dodson, A. H. Goldkamp and R. D. Muir, J. Amer. Chem. Soc. 82 4026 (1960)].
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- Aminodesoxy-1.4;3.6-dianhydrohexitol nitrates and pharmaceutical composition
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Aminodesoxy-1.4;3.6-dianhydrohexitol nitrates of the general formula I, STR1 wherein R1 and R2 possess the meanings given in claim 1, as well as their pharmacologically acceptable acid-addition salts; processes for the preparation of said compounds, and pharmaceutical compositions containing at least one of said compounds.
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- Methanesulfonamides as antistatic agents for laundered fabrics
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Novel methanesulfonamides useful as non-yellowing antistatic agents for laundered fabrics, detergent compositions containing an effective anti-static amount of said methanesulfonamide and a method of protecting fabrics against acquiring static electricity by contacting fabrics with said composition during laundering. These compounds provide antistatic protection without reducing optical brightener performance of the detergent composition. This invention relates to novel antistatic agents and detergent compositions to be used in the laundering of fabrics containing said antistatic agent which is a nitrogen substituted methansulfonamide having the formula: wherein R is a secondary aliphatic hydrocarbon chain of at least 8 carbons.
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- Process for preparing amides by reaction in presence of molecular sieve
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There is provided a process for preparing amides which comprises reacting an amine, or an amide, and an acid halide, or anhydride, in suitable molecular proportions, in an inert organic diluent, in the presence of an effective amount of a molecular sieve, until the reaction is completed, separating the molecular sieve, and recovering the amide from the organic mother liquor.
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- Phosphoric acid esters, composition and use
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Phosphoric (phosphonic) acid esters of the formula STR1 where R1 denotes linear or branched alkyl of up to 4 carbon atoms, R2 denotes linear or branched alkyl, alkoxy or alkylthio, each of up to 4 carbon atoms, mono- or dialkylamino of up to 4 carbon atoms in each alkyl, or phenyl, R3 denotes linear or branched alkoxy or alkylthio of up to 4 carbon atoms, amino, mono- or dialkylamino of up to 4 carbon atoms in each alkyl, alkylalkoxyalkylamino of up to 4 carbon atoms in each alkyl or alkoxyalkyl, dialkoxyalkylamino of up to 4 carbon atoms in each alkoxyalkyl, alkylalkenylamino of up to 4 carbon atoms in each alkyl or alkenyl, alkylalkynylamino of up to 4 carbon atoms in each alkyl or alkynyl, N-methyl-N-methoxyamino, N-(2-methoxyethyl)-N-(2-cyanoethyl), a 5- or 6-membered nitrogenous heterocyclic ring which may contain several nitrogen atoms and optionally oxygen as ring members, R4 denotes unsubstituted or halogen-substituted acyl of up to 4 carbon atoms, alkylsulfonyl or haloalkylsulfonyl of up to 4 carbon atoms in each alkyl or haloalkyl, the group --CO--NR5 R6, R5 and R6 denoting hydrogen, linear or branched alkyl of up to 4 carbon atoms, or - but not simultaneously - phenyl, or R5 and R6 denoting, together with the nitrogen atom whose substituents they are, a 5- or 6-membered heterocyclic ring with further nitrogen atoms and an oxygen atom as ring members, or R4 denotes the group --CO--Y--R7, R7 denoting linear or branched alkyl of up to 4 carbon atoms, phenyl or benzyl, and Y denoting oxygen or sulfur, and X denotes oxygen or sulfur, which are effective against pests, especially insects, mites and ticks; pesticides containing these phosphoric (phosphonic) acid esters as active ingredients; a process for producing these active ingredients; and a process for combating pests with these active ingredients.
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- DIMETHYLSULPHOXIDE ADDUCTS WITH CHLORINATED LEWIS ACIDS AND WITH CHLORINE: NMR INVESTIGATIONS
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The structure and mechanism of formation of the ionic species formed in the reaction of dimethylsulfoxide with COCl2, POCl3, PCl5, Cl2CHOCH3, (CH3)2N=CHCl(1+), Cl(1-) or OPOCl(2-), and Cl2 are studied by proton, carbon and phosphorus NMR.
- Gouvreau, J. R.,Poignant, S.,Martin, G. J.
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p. 1319 - 1322
(2007/10/02)
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