cas 636-70-4, TRIETHYLAMINE HYDROBROMIDE | Articles data

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Palladium-Catalyzed Hydride Addition/C-H Bond Activation Cascade: Cycloisomerization of 1,6-Diynes
The use of ammonium halide salts as metal hydride precursors in a new Pd-catalyzed cycloisomerization of 1,6-diynes, which affords unexplored silylated 2-azafluorenes, is reported. This cascade process includes the addition of a Pd-hydride species to a π-system, intramolecular carbopalladation, and C(sp2)-H bond activation. A variety of functional groups are tolerated, and the synthetic utility of the resulting products has been demonstrated by a series of derivatizations.
Rodríguez, José F.,Burton, Katherine I.,Franzoni, Ivan,Petrone, David A.,Scheipers, Ina,Lautens, Mark
supporting information
p. 6915 - 6919
(2018/11/21)

Deactivation of the coordinating ability of the iminophosphorane group by the effect of ortho-carborane
The C-carboranyl iminophosphorane compounds derived from triphenylphosphine (I1) and o-(methylthiophenyl)-diphenylphosphine (I2) were obtained and structurally characterized. Functionalization with sulfur on the other cage carbon atom gave the correspondi
Crujeiras, Pablo,Rodríguez-Rey, José Luis,Sousa-Pedrares, Antonio
p. 2572 - 2593
(2017/03/08)

A highly fluorescent cationic bifunctional conjugate
It was of crucial importance to modify perylene-3,4,9,10-tetracarboxylic acid bisimides (PBIs) for the design of new perylene-based bio-dye agents with strong fluorescence. Recently, we reported that ethanolamine (EA)-functionalized poly(glycidyl methacrylate) (or PGEA) can produce good transfection efficiency, while exhibiting very low toxicity. Herein, the low-toxic PGEA was proposed to be conjugated with PBIs via facile atom transfer radical polymerization for the well-defined highly fluorescent cationic bifunctional conjugate (PBI-PGEA). The obtained PBI-PGEA exhibited good water-solubility properties, characteristic spectroscopic patterns of PBIs, and excellent photostability. The PBI-PGEA conjugate can be used as an efficient cell bio-dye for rapid (2-5 min) cell labeling at low concentrations (0.06-0.12 mg mL-1). Such a fast labeling process did not induce obvious cytotoxicity, avoiding possible side-effects to the cells. In addition, the PBI-PGEA still possessed good gene transfection efficiency in different cell lines. With the strong fluorescence in water and good transfection properties, the developed bifunctional PBI-PGEA should possess more potential in bioimaging and gene delivery.
Yang,Chai,Zhu,Yang,Xu
experimental part
p. 7806 - 7812
(2012/08/13)

Preparation of biocompatible sterically stabilized latexes using well-defined poly(2-(methacryloyloxy)ethyl phosphorylcholine) macromonomers
A range of well-defined methacrylic macromonomers based on the biomimetic monomer 2-(methacryloyloxy)ethyl phosphorylcholine (MPC) were synthesized by atom-transfer radical polymerization (ATRP) in alcoholic media using 2-(dimethylamino)ethyl-2-bromoisobutyrylamide. This tertiary amine-functionalized initiator was used to produce homopolymer precursors of various chain lengths via ATRP. These polymerizations were relatively well controlled (Mw/Mn ≤ 1.30), provided that the target degree of polymerization (DP) did not exceed 30. For higher target DPs, polymerization was only poorly controlled and characterized by broad molecular weight distributions (Mw/Mn = 1.50-2.31). The tertiary amine end-group of each nearly monodisperse homopolymer precursor was then quaternized using 4-vinylbenzyl chloride (4-VBC) to afford the corresponding styrene-functionalized macromonomers. PMPC30 macromonomer proved to be an effective reactive steric stabilizer for the formation of polystyrene latexes when employed at 10 w/w % on the basis of the styrene monomer. Nearly monodisperse submicrometer-sized and micrometer-sized latexes were prepared by aqueous emulsion and alcoholic dispersion polymerization, respectively, as judged by scanning electron microscopy and dynamic light scattering studies. In contrast, attempted alcoholic dispersion polymerization conducted either in the presence of the PMPC30 homopolymer precursor or in the absence of any macromonomer always resulted in macroscopic precipitation. Such control experiments confirmed the importance of the terminal styrene groups on the macromonomer chains for successful latex formation. FTIR spectroscopy indicated the presence of the PMPC30 macromonomer within the polystyrene latex, and XPS studies indicated that these stabilizer chains are located at (or very near) the latex surface, as expected. Using PMPC20 and PMPC 10 macromonomers for the alcoholic dispersion polymerization of styrene led to latexes with substantially broader size distributions compared to those produced using the PMPC30 macromonomer under the same conditions. Finally, these new sterically stabilized latexes exhibit excellent freeze-thaw stability and salt tolerance.
Thompson, Kate L.,Bannister, Iveta,Armes, Steven P.,Lewis, Andrew L.
experimental part
p. 4693 - 4702
(2010/11/18)

Synthesis and molluscicidal evaluation of some new pyrazole, isoxazole, pyridine, pyrimidine, 1,4-thiazine and 1,3,4-thiadiazine derivatives incorporating benzofuran moiety
Chalcone derivative 3 was synthesized via the base catalyzed Claisen-Schmidt condensation and was used as a precursor for synthesizing pyrazoline 11, isoxazoline 12, pyrazoline carbothioamide 13, 5,6-dihydropyrimidine-2-(1H)-thione 14 and aminopyridinecarbonitrile derivative 15. Bromination of 3 afforded the dibromo derivative 4. Monobromo derivative 5 obtained by boiling 4 in dry benzene in the presence of triethylamine. Fused thiadiazines 9a,b and 1,4-thiazine 9c derivatives were synthesized upon treatment of α-bromopropenone derivative 5 with 4-amino-4H-1,2,4-triazole- 3-thiol (6) or 1-amino-2-mercapto-5-methylpyrimidin-4(1H)-one (7) or with 2-aminothiophenol (8) in ethanolic potassium hydroxide solution. The newly synthesized compounds were screened for their molluscicidal activities, whereas compounds 3, 4, 9a, 11 and 15 exhibited promising molluscicidal activities. On the other hand compounds 5, 9b, 9c, 12, 13 and 14 showed a moderate effect as compared to the standard molluscicidal agent (Bayluscide).
El Shehry,Swellem,Abu-Bakr, Sh.M.,El-Telbani
experimental part
p. 4783 - 4787
(2010/11/17)

HETEROCYCLIC AROMATIC COMPOUNDS
New classes of heterocyclic aromatic cationic compounds are disclosed, and in particular new classes of phenanthridinium derivatives, most notably dihydro-imidazo-phenanthridinium (DIP) compounds. These findings are based on the reaction of the middle b ring of a phenanthridinium core with primary amines to form DIP compounds (Formula A) or secondary amines to form 2-aminoalkyl phenanthridinium derivatives (Formula B). These reactions can also be applied to other classes of starting compounds which comprise a 6-membered ring aromatic heterocycle having a ring nitrogen and at least one alpha hydrogen atom which can be reacted with a primary or secondary amine.
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Page/Page column 65; 87-89

(2008/06/13)

Technetium or rhenium complexes, radiopharmaceutical products comprising them
The invention relates to a technetium or rhenium complex of formula (I): [in-line-formulae][M (R1CS3)2L]??(I) [/in-line-formulae] in which M is Tc or Re, R1 represents an alkyl, cycloalkyl, aralkyl or aryl group which is unsubstituted or substituted by one or more substituents chosen from halogen atoms, the hydroxyl group, alkyl groups and alkoxy groups, and L is a dithiolate ligand, with the exception of the ligand of formula R2CS2 in which R2 is identical to R1. The dithiolate ligand is preferably a dithiocarbamate. The invention also relates to a radiopharmaceutical product comprising a complex of formula (I) with M representing 99Tc, 186Re or 188Re.
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Page 8

(2010/02/10)

LIQUID CRYSTAL COMPOUND COMPRISING TWO CONDENSED AND SUBSTITUTED RINGS
A new liquid crystal compound comprises two condensed and substituted rings. The ring preferably is a five-membered heterocyclic ring. The heterocyclic ring is preferably condensed with benzene ring or an aromatic six-membered heterocyclic ring. The benzene ring or the aromatic six-membered heterocyclic ring is preferably substituted with a group comprising a cyclic structure and a chain structure. The liquid crystal compound is advantageously used in preparation of a thin phase retarder, such as a wide-ranged l/4 plate, which gives inverse wavelength distribution. The phase retarder can be easily produced according to a simple process by using the new liquid crystal compound.
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Page/Page column 83-84

(2008/06/13)

NEW CYANATE ESTER AND METHOD FOR PRODUCING THE SAME
PROBLEM TO BE SOLVED: To provide a new cyanate ester having high storage stability by itself and affording a plastic having excellent light transmittance and heat resistance, low values of permittivity and dielectric dissipation factor and a high refractive index and resultantly useful in, e.g. applications of optical techniques by using the cyanate ester as a raw material and to provide a method for producing the cyanate ester. SOLUTION: The cyanate ester is represented by general formula (I) (wherein, R denotes a fluorenylidene group or a p-biphenylmethylidene group). The cyanate ester is obtained by reacting a bisphenol represented by general formula (II) (wherein, R denotes a fluorenylidene group or a p-biphenylmethylidene group) with a cyanogen halide represented by general formula (III) (wherein, X denotes a halogen atom).
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Page/Page column 11

(2008/06/13)

Synthesis and anti-tumor activity of nitrogen substituted thalidomide analogs
The present invention comprises a group of compounds that effectively inhibit angiogenesis. More specifically, nitrogen-substituted thalidomide analogs and di-substituted thalidomide analogs have been shown to inhibit angiogenesis. Importantly, these compounds can be administered orally.
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(2008/06/13)

Serotonin reuptake inhibitor
A serotonin reuptake inhibitor containing a cyclic amine represented by the following formula, a prodrug thereof, or a pharmaceutically acceptable salt of said cyclic amine or prodrug as an active ingredient: wherein R0 is a hydrogen atom, a halogen atom, an alkyl group, a substituted alkyl group, a hydroxyl group, an alkoxy group or the like, R3 is a hydrogen atom or the like, Y is an alkylene group or the like, Z is a hydrogen atom, a cycloalkyl group, an aryl group or the like, n is 1, 2 or 3, and m is 2, 3, 4, 5 or 6.
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(2008/06/13)

Use of molecular weight-enlarged catalysts in a process for asymmetric, continous hydrogenation, novel molecular weight-enlarged ligands and catalysts
The first embodiment of the present invention provides a process, which includes: in a continuous process in a membrane reactor, asymmetrically hydrogenating at least one C=C, C=N or C=O double bond with a catalyst. Another embodiment of the present invention provides a ligand, which includes at least one di-1,3-aminophosphine homochiral active center; optionally, a linker; and a molecular weight-enlarging polymer; wherein the active center is bound to the molecular weight-enlarging polymer through the linker or is bound directly to the molecular weight-enlarging polymer; and wherein the linker is defined in the claims. Another embodiment of the present invention provides a process for preparing the above-noted ligand, and a catalyst that includes the above-noted ligand.
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(2008/06/13)

Synthesis of bridgehead nitrogen heterocycles via cyclization of α- ammonio 5-hexenyl radicals
Ring-closure of the 2,2-dimethyl-2-azonia-5-hexenyl radical (4) proceeds smoothly and efficiently to give the 5-exo isomer essentially quantitatively, in accordance with predictions based on MP4SDTQ/6-31G* ab initio calculations on the thermodynamic stability of α-ammonio radicals. The corresponding 5-hexynyl radical species 15 and its 6-phenyl derivative 19 display similar behavior affording the analogous 5-exo-3- methylenepyrrolidinium salts in high yield. In none of these cases were the products of reduction were detected. All of the radical intermediates were generated conveniently by treatment of the iodomethyl and/or phenylselenomethyl salts with tributyltin hydride. Application of this procedure to monocyclic precursors such as 1-methyl-1-iodomethyl-4-methylene- 1-azoniacyclohexyl iodide (31) provided an attractive entry into quaternary derivatives of the 1-azabicyclo[2.2.1]heptyl system in good yield via a three-step sequence from 1-methylpiperidone. Dequaternization of the bicyclic salts so obtained unexpectedly leads to rupture of one of the rings rather than loss of the N-methyl group. The 1-azabicyclo[2.2.1]heptane could be accessed readily via tin hydride-induced cyclization of the corresponding N- phenylethylammonium salt 54, followed by Hofmann elimination with potassium tert-butoxide.
Della, Ernest W.,Smith, Paul A.
p. 1798 - 1806
(2007/10/03)

Process for preparing aromatic acetylenes using palladacycles as catalysts
The invention relates to a process for preparing aromatic acetylenes of the formula (I): Ar--C C--R8a, where Ar is: STR1 by reacting haloaromatics or aryl sulfonates of the formula (II): Ar--X, with monosubstituted acetylenes of the formula (III): Ar--C C--R8a, where Ar is defined above and X is bromine, chlorine or OSO2 R, in the presence of a palladium compound catalyst of the formula (IV): STR2 where R1, R2, R3, R4, R5, R6 are, independently of one another, hydrogen (C1 -C4)-alkyl, (C1 -C4)-alkoxy, fluorine, NH2, NH-alkyl-(C1 -C4), N(alkyl)2 -(C1 -C4), CO2 -alkyl-(C1 -C4), OCO-alkyl-(C1 -C4), or phenyl, or R1 and R2, R2 and R3, R3 and R4, R5 and R6, together form an aliphatic or aromatic ring, and R7, R8 are (C1 -C8)-alkyl, (C3 -C12)-cycloalkyl, substituted or unsubstituted aryl, and Y is an anion of an inorganic or organic acid.
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(2008/06/13)

Production of racemic 2-(6-methoxy-2-naphthyl) propionic acid of precursors thereof
In producing (±)-2-(6-methoxy-2-naphthyl)propionic acid or precursor thereof from 2-bromo-6-methoxynaphthalene, use is made of 2-bromo-6-methoxynaphthalene formed by (a) methylating 6-bromo-2-naphthol with methyl chloride in a solvent comprising one or more compounds, RZ, where R is a hydrogen atom or an alkyl group, and Z is --OH or --CN provided that if Z is --CN, R is alkyl, and in the presence of a strong base; and (b) recovering and purifying 2-bromo-6-methoxynaphthalene so formed. Preferably, the 6-bromo-2-naphthol is formed by (1) reacting 1,6-dibromo-2-naphthol with hydrogen, in a solvent comprising (a) organic halide in which the halogen has an atomic number of 35 or less or (b) a mixture of water and such organic halide, and in the presence of catalytically effective amounts of (i) a tungsten carbide-based catalyst, and (ii) phase transfer catalyst; and (2) separating 6-bromo-2-naphthol from the organic halide solvent so that the 6-bromo-2-naphthol is substantially free of halogen-containing impurities before use in the above methylation reaction. This technology makes possible reductions in quantities of co-products formed, eliminates need for use of excess iron and/or dimethyl sulfate as reaction components, and makes possible improvements in plant operating efficiency. Precursors of (±)-2-(6-methoxy-2-naphthyl)propionic acid formed from such 2-bromo-6-methoxynaphthalene are Grignard reagent of 2-bromo-6-methoxynaphthalene, bis(6-methoxy-2-naphthyl)zinc, 6-methoxy-2-naphthylzinc halide, 6-methoxy-2-naphthyllithium, 6-methoxy-2-naphthylcopper(I), bis(6-methoxy-2-naphthyl)cadmium, 6-methoxy-2-naphthylcadmium halide, and 6-methoxy-2-vinylnaphthalene.
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(2008/06/13)

Cyclopropyl derivatives, preparation method there-of and applications
Cyclopropyl derivatives of formula (I) wherein R is cyclopropyl or methyllopropyl are prepared by reaction of 2,6-dibromohexanoyl chloride with 2,6-dimethylaniline in the presence of a base at 0°-25° C. to give 2,6-dibromohexanoyl-2,6-dimethylanilide which subsequently is reacted with R--NH2 (wherein R is cyclopropyl or methylcyclopropyl) at 70°-100° C. The compounds are useful as antiarrhythmic agents and as local anaesthetic agents.
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(2008/06/13)

Reaction of N-alkylpyredinium salts with phosphorus trichloride
1-Alkylpyridinium bromides 1 having activated N-methylene group react with phosphorus trichloride to give N-(dichlorophosphinomethylene)pyridinium ylides 2. The site of the reaction in 1,2-dialkylpyridinium halides 3 under these conditions is determined by the relative activation of 1- and 2-methylene groups; in the absence of sufficient activation of N-methylene group, reaction occurs at the 2-methylene group to give dichlorophosphinylated anhydrobases 5 and 11. 1,4-Dialkylpyridinium bromide 13 behaves analogously to give the corresponding dichlorophosphinylated anhydrobase 14.
Bansal, Raj K.,Gupta, Neelima,Gupta, Rakhi,Pandey, Garima,Agarwal, Mamta
p. 121 - 130
(2007/10/03)

R,R,S,S-2-nitroimidazole derivatives
High purity 2-nitroimidazole derivatives having excellent radiosensitivity and high safety and useful as a drug to be used along with radiotherapy of various cancers can be prepared at a high yield from inexpensive diester of tartaric acid according to the following reaction formua, STR1 wherein R1 and R2 may be the same or different and each individually represents an aliphatic group or an aromatic group, and X represents a halogen atom.
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(2008/06/13)

(Aryl(alkyl)carbonyl)-heterocyclic compounds, compositions and use
The invention relates to a compound selected from those of formula (I): STR1 wherein Ar, n, B and A are as defined in the description, to their optical isomers, and to their addition salts there of with a pharmaceutically-acceptable acid or base. Medicinal product which is useful for treating pain and treating or preventing pathologies which require psychotropic agents.
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(2008/06/13)

Substituted cyclohexane derivatives, processes for their preparation and the use of the compounds for treating diseases
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(2008/06/13)

N-cyanoimides
Polyfunctional N-cyanoimides and their precursors and derivatives are disclosed along with methods for their preparation and interconversion. Also disclosed are curable compositions comprising the N-cyanoimides or poly(amide-cyanoamides) and reactive diluents as well as novel dianhydrides, polyimides, and poly(amide-cyanoamides) and methods for making them.
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(2008/06/13)

Salts of 3-azabicyclo [3.3.1]nonanes as antiarrhythmic agents, and precursors thereof
Salts of 3-azabicyclo[3.3.1]nonanes are used in controlling antiarrhythmic processes and precursors thereof are disclosed.
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(2008/06/13)

Salts of 3-azabicyclo[3.3.1]nonanes as antiarrhythmic agents, and precursors thereof
Salts of 3-azabicyclo[3.3.1]nonanes are used in controlling antiarrhythmic processes and precursors thereof are disclosed.
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(2008/06/13)

N-amino bicyclic compounds
N-amino hexahydrocyclopenta imidazole-2(1H)-one derivatives useful for treating or preventing thrombo-embolic disorders and ocular diseases characterized by increased ocular pressure.
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(2008/06/13)

Novel polyphenol and thermosetting plastics prepared therefrom
Novel phenol compounds of the general formula STR1 where X is a sulfone group or contains a sulfone group, are suitable for the preparation of epoxy resins, vinyl ester resins, bismaleimide resins and cyanate resins.
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(2008/06/13)

Synthesis, properties, and structural investigations of 1,3,2-diazaborolidines and 2,3-dihydro-1H-1,3,2-diazaboroles
A series of variously substituted 1,3,2-diazaborolidines have been prepared by different methods. 1,3-Diisopropyl-2-methyl-1,3,2-diazaborolidine (1a), 1,3-diethyl-2-methyl-1,3,2-diazaborolidine (2a), 1-ethyl-2,3-dimethyl-1,3,2-diazaborolidine (3a), and 1,2,3-trimethyl-1,3,2-diazaborolidine (4a) are formed from the corresponding lithiated ethylenediamines and CH3BBr2 in diethyl ether (method C). 2-Methyl-1-(trimethylsilyl)-1,3,2-diazaborolidine (5a), 1-tert-butyl-2-methyl-1,3,2-diazaborolidine (6a), and 1-isopropyl-2-methyl-1,3,2-diazaborolidine (7a) can be prepared either by method C, by method A, using the ethylenediamines and H3CB[N(CH3)2]2 to eliminate HN(CH3)2, or by method B, starting with CH3BBr2, NR3, and the corresponding ethylenediamines. The unsaturated 2,3-dihydro-1H-1,3,2-diazaboroles 1b-7b are synthesized by catalytic dehydrogenation in either liquid (1b-3b) or gaseous (4b-7b) state. Diazaboroles can act as 6-π-electron donors in Cr(CO)3 complexes. 1b-4b react with (CH3CN)3Cr(CO)3 under various conditions to form the corresponding complexes 1c-4c. The monosubstituted rings 5b-7b are not suited to form stable Cr(CO)3 complexes. One of the two rings in 8 can be combined with a Cr(CO)3 fragment to give 9. The yellow 1H-1,3,2-diazaborole-tricarbonylchromium complexes 1c-4c decompose slowly at room temperature. 2,3-Dihydro-2-methyl-1,3-bis(trimethylsilyl)-1H-1,3,2-diazaborole (10) can be metalated at one N atom by NaNH2 and K(O-t-Bu) to give the salts 11a and 11b. These alkali-metal derivatives can easily be protonated by HCl or CH3OH to form the N-H derivative 5b. X-ray structure analyses have been performed on the diazaborolidines 2a and 4a and on the diazaboroles 1b, 2b, 4b, and 8. The structures of 2a and 4b have been determined at two different temperatures. 1b, 2b, and 2a crystallize in the monoclinic space groups P21/n, P21/c, and Cc, respectively. 4a crystallizes hexagonally in the space group P32; 4b, tetragonally in the space group P42. X-X-Difference electron densities of 4a, 2a, and 4b show that the B-N bonds in the saturated compounds 4a and 2a possess remarkable double-bond character. The electron distribution in the 1,3,2-diazaborole 4b corresponds with that in 6-π-electron systems.
Schmid, Günter,Polk, Michael,Boese, Roland
p. 4421 - 4429
(2008/10/08)

(2-cyano-2-oximinoacetyl)-amino acid derivatives
Novel fungicidally active compounds of the formula STR1 in which R represents alkyl, cyanoalkyl or in each case optionally substituted alkenyl, alkinyl, cycloalkyl, cycloalkylalkyl or phenylalkyl, R1 represents the --OR2 or --NR3 R4 groups, and R3 and R4 have special special definitions.
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(2008/06/13)

Phenylacetylene-substituted schiff's base momomers and electroconductive polymers
Novel mono- or difunctional phenylacetylene-substituted Schiff's base monomers useful in the preparation of electrically conducting polymers is disclosed. On heating, these monomers melt to a viscous liquid state, and on continued heating above about 300°C polymerize to form an electrically insulating thermoset polymer. On further post-cure heat treatment, the polymer becomes electroconductive showing a bulk conductivity of at least 10 2 S/cm.
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(2008/06/13)

ARALKYLAMINOETHANOL HETEROCYCLIC COMPOUNDS
Heterocyclic aminoethanols of the formula: Het--CHOH--CH 2--NH-aralkylwhere Het is a 6-10 membered N-heterocycle are disclosed. The compounds are useful as pharmaceuticals.
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(2008/06/13)

Process for preparing carboxyalkyl dipeptides
Pharmaceutically active carboxyalkyl dipeptides such as enalapril, lisinopril and the like, are prepared from a starting amino acid such as L-alanine, by protecting the acid function of the amino acid with an alkyl silyl protecting group, while it is reacted with an α-halo ester, at its amino function. Subsequently, the silyl protectant is removed, and the acid group is reacted with the amino function of an appropriate amino acid such as L-proline, to form the dipeptide product.
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(2008/06/13)

6-(1-CARBAMOYL-1-HYDROXYMETHYL)PENICILLANIC ACID DERIVATIVES
6-(1-Carbamoyl-1-hydroxymethyl)penicillanic acid derivatives are useful as antibacterials and/or beta-lactamase inhibitors.
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(2008/06/13)

Haloalkyl complexes of the transition metals VI. A study of the reactions of halomethyldicarbonylcyclopentadienyliron complexes with some tertiary phosphine, amine and sulphur ligands
The reactions of with a series of tertiary phosphines, amines, and SMe2 have been investigated in both CH3CN and THF (Cp=Η5-C5H5 and X=Cl, Br or I).Two types of cationic products, namely the ylide complexes +
Bellinger, Geoffrey C. A.,Friedrich, Holger B.,Moss, John R.
p. 175 - 186
(2007/10/02)

Nitrodibromoacetonitrile: An Agent for Bromination and for the Formation of Adducts Formally Derived from Cyanonitrocarbene
The reactions of nitrodibromoacetonitrile (NDBA) with alkenes, aromatic compounds, amines, and sulphides have been studied.Products were formally derived from bromine or nitrocyanocarbene except for bis(2-bromocyclohexyl)nitroacetonitrile (13), an adduct (2:1) obtained from cyclohexene and NDBA. 2,3-Dimethylbut-2-ene was converted into 3-cyano-4,4,5,5-tetramethyl-4,5-dihydroisoxazole 2-oxide (15) and 2,3-dibromo-2,3-dimethylbutane (16). meso-1,2-Dibromo-1,2-diphenylethane was obtained from trans-stilbene.In a reaction catalysed by copper, benzene and NDBA gave benzoyl cyanide.From anthracene, phenol, and cupric acetylacetonate, 9,10-dibromoanthracene, 4-bromophenol, and cupric bromoacetylacetonate were obtained respectively.Dimethyl sulphide, tetrahydrothiophene, and triethylamine afforded the corresponding sulphonium-(30) and (31) and ammonium cyanomethylide-(33) derivatives and, with the latter, co-formation of triethylammonium bromide.Rationales for the reactions are discussed.
Boyer, Joseph H.,Manimaran, Thanikavelu
p. 1381 - 1385
(2007/10/02)

2-oxo-4-carboxy-pyrimidines and their use as anti-malaria and anti-cancer agents
A compound for use as an inhibitor for the enzyme dihydroorotase and which is of general formula (I) STR1 where either (i) A and B together are =S or (ii) A is --H, and B is --COR2 or --SR6 ; and R1 and R2 which may be the same or different are --OH; alkyloxymethyl, a di-, tri- or polypeptide group, --OR where R is saturated or unsaturated C1-16 alkyl, C1-16 alkyloxymethyl, or 4-alkyl-piperidinyl-alkyl, --NR'R' where each R' is independently selected from --H, saturated or unsaturated C1-16 alkyl, or any group above to be hydrolyzed in vivo to hydroxy; R3 and R4 which may be the same or different are --H, C1-6 alkyl, hydroxy C1-16 alkyl, hydroxy C1-6 ether group, tetrahydrofuranyl, tetrahydropyranyl, a sugar or acetylated sugar group, hexylcarbamyl, methylglycine-N-carbonyl, or any group able to be hydrolyzed in vivo to --H; R5 is --H, halo, or C1-6 alkyl; R6 is C1-6 alkyl or 1-methyl-4-nitroimidazol-5-yl; and the dotted line represents a double bond which may be absent or present in the 4-5 position. The compounds are useful as anti-cancer and anti-malarial drugs.
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(2008/06/13)

2-Oxo-4-carboxy-pyrimidines
A compound for use as an inhibitor for the enzyme dihydroorotase and which is of general formula (I) where either (i) A and B together are =S, or (ii) A is -H, and B is -COR2 or -SR6; and, R1 and R2 which may be the same or different are -OH; alkyloxymethyl, a di-, tri- or polypeptide group, -OR where R is saturated or unsaturated C1-16alkyl, C1-16alkyloxymethyl, or 4-alkyl-piperidinyl-alkyl, -NR′R′ where each R′ is independently selected from -H, saturated or unsaturated C1-16alkyl, or any group able to be hydrolysed in vivoto hydroxy;, R3 and R4 which may be the same or different are -H, C1-6alkyl, hydroxy C1-16alkyl, hydroxy C1-6ether group, tetrahydrofuranyl, tetrahydropyranyl, a sugar or acetylated sugar group, hexylcarbamyl, methylglycine-N-carbonyl, or any group able to be hydrolysed in vivoto -H;, R5 is -H, halo, or C1-6alkyl;, R6 is C1-6alkyl or 1-methyl-4-nitroimidazol-5-yl; and the dotted line represents a double bond which may be absent or present in the 4-5 position. The compounds are useful as anti-cancer and anti-malarial drugs.
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(2008/06/13)

Sparingly soluble salts of cefamandole, and ophthalmic compositions containing same
The hydrabamine and benzathine salts of cefamandole are useful in aqueous ophthalmic compositions which have good stability and shelf life.
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(2008/06/13)

Process for the preparation of ethynylbenzaldehydes
A multi-step process for the preparation of ethynylbenzaldehydes from bromo- or iodobenzaldehydes is disclosed. The arylhalogen is replaced with a protected ethynyl compound which is subsequently cleaved by base to form the arylacetylene. The aldehydic functionality is preserved by formation of a corresponding Schiff's base or acetal, and its subsequent regeneration by treatment with aqueous acid.
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(2008/06/13)

Certain pyridyl, thienyl or furyl propenoic acids or esters having anti-inflammatory anti-allergic properties
Compounds of formula (I): STR1 in which R1 is hydrogen or C1-6 alkyl; R2 is hydrogen or a group --CO2 R3 where R3 is hydrogen or C1-6 alkyl; n is an integer of from 2 to 12; X represents a double or triple bond, and each of A and B represents hydrogen when X is a double bond, or both A and B are absent when X is a triple bond; and STR2 represents an aromatic heterocyclic ring, are disclosed as inhibitors of 5-lipoxygenase.
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(2008/06/13)

AMINOLYSIS OF VINYLAMMONIUM SALTS. EFFECTS OF STRUCTURE AND MEDIUM
The kinetics of the aminolysis of a series of vinylammonium salts ZCH=CHN+R3*X- were investigated in polar solvents and in water at 25 deg C.A quantitative assessment was made of the effect of the nature of the medium and the structure of activating group Z on the rate of the investigated processes.The aminolysis rate of the salts increases with increase in the donating characteristics of the solvent on account of the greater stabilization of the transition state compared with the initial state.Increase in the accepting characteristics of the medium leads to retardation of the process as a result of increase in the electrophilic solvation of the amine in the initial state.
Kravchenko, V. V.,Popov, A. F.,Kotenko, A. A.
p. 1332 - 1336
(2007/10/02)

Derivatives of 1,1,2,2-tetramethyl-1,2-bis-(2-fluoro-4-hydroxyphenyl)-ethane
Antitumor compounds corresponding to the following formula: STR1 in which the substituents R1 and R2 may be the same or different and represent hydrogen, an aminocarbonyl group, a C1 -C6 alkylaminocarbonyl group, a di-C1 -C6 -alkylaminocarbonyl group, the group PO(OH)2, a C2 -C8 alkanoyl group, a C2 -C8 halogen alkanoyl group or a C3 -C8 alkenoyl group, a process for their preparation, and their use in treating oestrogen-receptor-positive-tumors as well as the prostate carcinoma.
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(2008/06/13)

Process for preparing triarylmethyl methacrylate
A triarylmethyl methacrylate is produced by reacting methacrylic acid with a triarylmethylating agent in an inert, organic solvent containing therein an excess amount of an amine or in the presence of an anion exchanger.
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(2008/06/13)

Infrared Spectroscopic Studies of Hydrogen Bonding in Triethylammonium Slats. Part 4. Rearrangement of Hydrogen-bonded Ion Pairs of Triethylammonium Salts caused by Interaction with Tetrabutylammonium Salts in Solution
Rearrangement of triethyl- and tetrabutylammonium salts in chloroform solution has been revealed from the characteristic features of the ν(N+H) bands caused by Fermi resonance interaction.Temperature changes of the i.r. spectra show this process to be reversible.Rearrangement constant K1 and K-1 and enthalpies -ΔH (for some cases only) of this process have been determined by measuring the total integrated intensities of the ν(N+H) bands of complexes which are in equilibrium.K1 values of the tetrabutylammonium salts increase with decreasing hydrogen bonding strength in triethylammonium salts.The measured enthalpies of rearrangement and those calculated from the ν(N+H) bands of hydrogen-bonded complexes studied are in agreement.It has also been shown that tetrabutylammonium salts anions can participate in the rearrangement of hydrogen-bonded ion pairs like the organic bases studied previously.
Mashkovsky, Alexander A.,Nabiullin, Ahat A.,Odinokov, Stanislav E.
p. 1879 - 1884
(2007/10/02)

KINETICS AND MECHANISM OF REACTION OF AMINES WITH β-BROMOPROPIOPHENONE
The reaction of β-bromopropiophenone with different amines in acetonitrile at 25 deg C was studied.It was found that in the case of primary and secondary amines, the end products of the reaction are β-aminopropiophenones, which form via the intermediate phenyl vinyl ketone.In the case of tertiary amines, the reaction ends at the stage of the formation of phenyl vinyl ketone.The reactivity of the amines in the formation of phenyl vinyl ketone is preferentially determined by their basicity.
Popov, A. F.,Piskunova, Z.,Matvienko, V. N.
p. 1299 - 1302
(2007/10/02)

Substituted propargyloxyacetonitrile derivatives, process for production thereof, and herbicide and agricultural-horticultural fungicide comprising said derivatives as active ingredients
Substituted propargyloxyacetonitrile derivative represented by the general formula (I) STR1 wherein R represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower haloalkyl group, a lower alkoxy group, a methylenedioxy group, a nitro group or a cyano group, n represents an integer of 1 to 5 and when n is an integer of 2 or more, R's may be identical or different, R1 represents a hydrogen atom or a lower alkyl group, and R2 represents a hydrogen atom, a lower alkyl group, a lower haloalkyl group or a halogen atom, provided that R1 and R2 are not simultaneously hydrogen atoms. The compounds have herbicidal and fungicidal activities.
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(2008/06/13)

Process for the preparation of 5-(2-bromovinyl)-uridine
The invention relates to (E)-5-(2-bromovinyl)-uridine and its derivatives of general formula VI, STR1 wherein R1 stands for a hydrogen atom, C1-8 alkanoyl group, benzoyl group or a benzoyl group substituted in para position either with a C1-4 alkyl group or a halogen atom, and a process for preparing them by brominating 2',3',5'-tri-O-acyl-5-ethyl-uridine of general formula IV, STR2 wherein R is identical with R1, except where R1 stands for a hydrogen atom, dehydrohalogenating the resulting dibromo compound of general formula V STR3 and optionally deacylating it. The resulting compounds of general formula VI are exhibiting significant potency against Herpes simplex virus species and are of remarkably low acute toxicity.
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(2008/06/13)

5-(Straight chain 3-12 carbon alkoxy)-8-quinolinamines and their use for treatment of malaria
Improved means for the chemotherapy of malaria have been achieved with 5-oxy-primaquine analogues having the formula: STR1 wherein R4 represents hydrogen or a methyl grouping, and R represents an alkyl group containing 3 to 12 carbon atoms and pharmaceutically acceptable salts thereof, wherein the salt-forming acid may be organic or inorganic in nature. These primaquine-related compounds afford improvement in the chemotherapy of malaria by exerting plasmodicidal action on malaria parasites which may be present in either the blood, formed tissues, or blood and formed tissues of the mammalian host. Such broad and practical spectrum of effectiveness distinguishes the said primaquine analogues, which may be administered parenterally or perorally to infected animals.
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(2008/06/13)

Heterocyclic compounds containing an alkoxycarbonyl and a substituted methyl group
The invention relates to new heterocyclic compound containing an alkoxycarbonyl and a substituted methyl group a process for the preparation of these and analogeous compound and pharmaceutical compositions containing them. More particularly, the invention concerns compounds of the general formula (IVa) STR1 wherein R' is hydrogen, 2-ethoxycarbonylethyl, aryl or a group suitable for a temporary protection of amides and Y' represents a group of the formula --COOZ or --CH2 M, in which Z is lower alkyl and M is hydroxyl, halogen, cyano or a group of the formula --O--SO2 R2, in which R2 is lower alkyl or aryl, with the proviso that if R' is phenyl, Y' cannot stand for the group --COOC2 H5. The invention further relates to a process for the preparation of compounds of the general formula (IV) STR2 in which R and Y are identical with R' and Y', respectively, except the proviso. According to a further aspect of the invention there are provided pharmaceutical compositions, first of all with antihypoxic activity, comprising compounds of the general formula (IVa) as active ingredient.
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(2008/06/13)

1-[3-(3,4,5-Trimethoxyphenoxy)-2-hydroxy-propyl]-4-aryl-piperazine-derivatives having pharmaceutical activity
There are prepared compounds corresponding to the general formula STR1 in which R1 is a hydrogen atom, a C2 to C6 -alkanoyl group, a C3 to C6 -alkenoyl group, a C3 to C6 -cycloalkyl carbonyl group, a benzoyl group, an alkoxybenzoyl group, a nicotinoyl group, a thienyl carbonyl group, a furyl carbonyl group, a phenylacetyl group or a C1 to C4 -alkoxyphenyl acetyl group and R2 represents a phenyl, naphthyl or pyridyl group or such group substituted by the groups R3 and R4, the groups R3 and R4, which may be the same or different, each representing hydrogen, hydroxyl, fluorine, chlorine, bromine, a nitro group, a trifluoromethyl group, a C1 to C6 -alkyl group, a C1 to C6 -alkoxy group, a C1 to C6 -alkyl thio group, a C1 to C6 -alkyl sulphonyl group, a C2 to C6 -alkanoyl group, an amino group, an acylamino group or an acyloxy group in which the acyl is of the type defined in respect to R1, and their salts. The compounds are pharmacodynamically active.
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(2008/06/13)

Method of preparing substituted benzaldehydes
A process for the preparation of Benzaldehydes substituted in the nucleus is disclosed by oxidation of the corresponding benzyl halides. The process is performed in the presence of water using aminoxides of tertiary amines.
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(2008/06/13)

2-Pyrrolidine methanol derivatives utilizable as medicaments
The compounds of the formula: STR1 in which X is a hydrogen or halogen atom or an alkoxy group having 1 to 4 carbon atoms, an alkyl or cycloalkyl group having 1 to 8 carbon atoms, and R represents a hydrogen atom, alkyl group having 1 to 4 carbon atoms, or an aralkyl or hydroxyalkyl group in which the alkyl chain has 1 to 4 carbon atoms are disclosed together with processes for their preparation and medicaments containing the compounds. These compounds are hypolipemiants. In addition, some of them are psychostimulants.
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(2008/06/13)