- Reactions of trimethylsilyl isocyanate with alcohols and phenols
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Mono-and diphenols add to trimethyl isocyanate on heating to give the corresponding aryl urethanes. Ethanol reacts with trimethylsilyl isocyanate to give ethyl urethane and ethyl allophanate in a ratio determined by reaction conditions.
- Pudovik,Krepysheva,Kharitonov,Pudovik
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Read Online
- CARBONYLATION OF 2 AND 2; A NEW SELECTIVE METHOD FOR PREPARATION OF
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Carbonylation of 2 (COD=1,5-cyclooctadiene) in ethanol gave the rhodium cluster selectively in high yield; when non polar solvents were used, the known 2 and 2 were obtained.Reaction of carbon monoxide with the isocyanato-bridged derivative 2 in ethanol also gave .In both cases the carbonylation reaction also gave NH2COOEt.Carbonylation of the iridium dichloride dimer 2 in the presence of sodium citrate gave .
- Monica, G. La,Monti, C.,Pizzotti, M.,Cenini, S.
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Read Online
- Preparation method of carbamate
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The invention belongs to the technical field of synthesis of amino and carboxyl compounds connected to the same carbon frame through urea alcoholysis, and particularly relates to a preparation methodof carbamate. The preparation method of the carbamate comprises the following steps of: sequentially introducing urea, alcohol and a catalyst into a reactor, sealing, and reacting at 90-120 DEG C for8-12 hours to obtain the carbamate, wherein the catalyst includes an alumina supported metal oxide. By adopting the method for preparation of the carbamate, the side reaction of urea decomposition canbe effectively avoided, impurities such as carbamate are not detected, and the yield of the carbamate is high.
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Paragraph 0041; 0045-0047
(2020/09/23)
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- Discovery of a dual tubulin polymerization and cell division cycle 20 homologue inhibitor via structural modification on apcin
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Apcin is one of the few compounds that have been previously reported as a Cdc20 specific inhibitor, although Cdc20 is a very promising drug target. We reported here the design, synthesis, and biological evaluations of 2,2,2-trichloro-1-aryl carbamate derivatives as Cdc20 inhibitors. Among these derivatives, compound 9f was much more efficient than the positive compound apcin in inhibiting cancer cell growth, but it had approximately the same binding affinity with apcin in SPR assays. It is possible that another mechanism of action might exist. Further evidence demonstrated that compound 9f also inhibited tubulin polymerization, disorganized the microtubule network, and blocked the cell cycle at the M phase with changes in the expression of cyclins. Thus, it induced apoptosis through the activation of caspase-3 and PARP. In addition, compound 9f inhibited cell migration and invasion in a concentration-dependent manner. These results provide guidance for developing the current series as potential new anticancer therapeutics.
- Huang, Pan,Le, Xiangyang,Huang, Fei,Yang, Jie,Yang, Haofeng,Ma, Junlong,Hu, Gaoyun,Li, Qianbin,Chen, Zhuo
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p. 4685 - 4700
(2020/06/08)
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- An Fe3O4@SiO2/Schiff base/Cu(ii) complex as an efficient recyclable magnetic nanocatalyst for selective mono: N-arylation of primary O-alkyl thiocarbamates and primary O-alkyl carbamates with aryl halides and arylboronic acids
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An efficient, convenient and novel method for the selective mono N-arylation of primary O-alkyl thiocarbamates and primary O-alkyl carbamates with aryl halides and arylboronic acids in the presence of a recyclable magnetic Cu(ii) nanocatalyst is described. A variety of mono N-arylated O-alkyl thiocarbamates and O-alkyl carbamates were prepared in good to excellent yields with a broad range of aryl coupling partners. The magnetic nanocatalyst can be easily recovered with an external magnetic field and reused at least five times without noticeable leaching or loss of its catalytic activity. This cost-effective and eco-friendly methodology has some other advantages, such as easy preparation of the catalyst, simple workup procedure, and easy purification, which makes this protocol interesting for the users in various fields of pharmacology and biotechnology systems.
- Sardarian, Ali Reza,Dindarloo Inaloo, Iman,Zangiabadi, Milad
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p. 8557 - 8565
(2019/06/14)
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- EXON SKIPPING OLIGOMER CONJUGATES FOR MUSCULAR DYSTROPHY
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Antisense oligomer conjugates complementary to a selected target site in the human dystrophin gene to induce exon 52 skipping are described.
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- A Physical Organic Approach to Tuning Reagents for Selective and Stable Methionine Bioconjugation
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We report a data-driven, physical organic approach to the development of new methionine-selective bioconjugation reagents with tunable adduct stabilities. Statistical modeling of structural features described by intrinsic physical organic parameters was applied to the development of a predictive model and to gain insight into features driving the stability of adducts formed from the chemoselective coupling of oxaziridine and methionine thioether partners through Redox Activated Chemical Tagging (ReACT). From these analyses, a correlation between sulfimide stabilities and sulfimide ν (C=O) stretching frequencies was revealed. We exploited the rational gains in adduct stability exposed by this analysis to achieve the design and synthesis of a bis-oxaziridine reagent for peptide stapling. Indeed, we observed that a macrocyclic peptide formed by ReACT stapling at methionine exhibited improved uptake into live cells compared to an unstapled congener, highlighting the potential utility of this unique chemical tool for thioether modification. This work provides a template for the broader use of data-driven approaches to bioconjugation chemistry and other chemical biology applications.
- Christian, Alec H.,Jia, Shang,Cao, Wendy,Zhang, Patricia,Meza, Arismel Tena,Sigman, Matthew S.,Chang, Christopher J.,Toste, F. Dean
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supporting information
p. 12657 - 12662
(2019/09/04)
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- Preparation method of (5-toluenesulfonyl-5H-pyrrolo[2,3-b]pyrazine-2-yl)ethyl carbamate
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The invention discloses a preparation method of (5-toluenesulfonyl-5H-pyrrolo[2,3-b]pyrazine-2-yl)ethyl carbamate, and belongs to the field of the chemical industry. The preparation method comprises the following steps: (1) preparation of N-ethyl carbamate: adopting ethanol as a solvent, performing a reaction on isocyanate and ethyl bromide zinc acetate at a molar ratio of 1:(2-3) at 35-40 DEG C for 6-8 hours under the protection of nitrogen, performing quenching with a saturated ammonium chloride solution after completion of the reaction, extracting the organic phase by using diethyl ether, and performing separation through column chromatography so as to obtain the target product; and (2) preparation of a mixed acid: adding fuming sulphuric acid with a mass concentration of 20-40% to sulfonic acid with a mass concentration of 50-70% so as to prepare the mixed acid. Through the preparation method, the preparation steps are reduced, the production cost is reduced, the production time issaved, the preparation efficiency is improved, and the preparation method is suitable for popularization and application.
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Paragraph 0012-0014
(2019/10/01)
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- Selective Synthesis of Secondary Arylcarbamates via Efficient and Cost Effective Copper-Catalyzed Mono Arylation of Primary Carbamates with Aryl Halides and Arylboronic Acids
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Abstract: An efficient, selective and cost-effective procedure has been developed for mono N-arylation of primary alkyl and benzyl carbamates with aryl iodides and bromides by incorporating CuI as an inexpensive and commercially available catalyst. Despite previous reports on C–N coupling reactions, this process does not need expensive ligands and takes advantage of readily available and inexpensive ethylenediamine (EDA) as the ligand. Reaction times were relatively short and related N-arylated carbamates were obtained in excellent yields. Interestingly, replacing CuI with Cu(OAc)2 allowed us to use arylboronic acids as coupling partner for this reaction. All products are well characterized by 1H- and 13C-NMR, MS, melting point, IR and CHNS techniques.
- Sardarian, Ali Reza,DindarlooInaloo, Iman,Zangiabadi, Milad
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p. 642 - 652
(2018/01/11)
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- Acid–base sites synergistic catalysis over Mg–Zr–Al mixed metal oxide toward synthesis of diethyl carbonate?
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In heterogeneous catalysis processes, development of high-performance acid–base sites synergistic catalysis has drawn increasing attention. In this work, we prepared Mg/Zr/Al mixed metal oxides (denoted as Mg2ZrxAl1x–MMO) derived from Mg–Zr–Al layered double hydroxides (LDHs) precursors. Their catalytic performance toward the synthesis of diethyl carbonate (DEC) from urea and ethanol was studied in detail, and the highest catalytic activity was obtained over the Mg2Zr0.53Al0.47MMO catalyst (DEC yield: 37.6%). By establishing correlation between the catalytic performance and Lewis acid–base sites measured by NH3-TPD and CO2-TPD, it is found that both weak acid site and medium strength base site contribute to the overall yield of DEC, which demonstrates an acid–base synergistic catalysis in this reaction. In addition, in situ Fourier transform infrared spectroscopy (in situ FTIR) measurements reveal that the Lewis base site activates ethanol to give ethoxide species; while Lewis acid site facilitates the activated adsorption of urea and the intermediate ethyl carbamate (EC). Therefore, this work provides an effective method for the preparation of tunable acid–base catalysts based on LDHs precursor approach, which can be potentially used in cooperative acid–base catalysis reaction.
- Yan, Tingting,Bing, Weihan,Xu, Ming,Li, Yinwen,Yang, Yusen,Cui, Guoqing,Yang, Lan,Wei, Min
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p. 4695 - 4702
(2018/02/07)
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- Fe3O4@SiO2/Schiff base/Pd complex as an efficient heterogeneous and recyclable nanocatalyst for chemoselective: N -arylation of O -alkyl primary carbamates
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An efficient, heterogeneous and cost effective method has been developed using an Fe3O4@SiO2/Schiff base/Pd complex as a magnetic and easily recyclable nanocatalyst for rapid and effective N-arylation of carbamates in good to excellent yield. The catalyst can be easily recovered and reused over six runs without significant decrease in the activity. Further highlights of this protocol are operational simplicity, versatility and relatively short reaction times.
- Sardarian,Zangiabadi,Inaloo, I. Dindarloo
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p. 92057 - 92064
(2016/10/11)
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- Process method of co-production of oxamide and carbamic acid ester through ammonia ester exchange method
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The invention discloses a process method of co-production of oxamide and carbamic acid ester through an ammonia ester exchange method. According to the process method, urea and oxalic acid diethyl serve as raw materials, and two products, namely the oxamide and the carbamic acid ester, can be obtained at the same time through a series of ammonia ester exchange reactions. By means of the process, the problems that products are singular, and by-products affect the reaction process in an original technology for synthesizing oxamide through oxalic acid diethyl ammonolysis and a technology for synthesizing carbamic acid ester through urea alcoholysis are solved; besides, due to the fact that urea is obtained through CO and NH synthesis, NH is replaced with urea, and the process method has active significance in converting CO into high added-value chemicals and efficiently utilizing CO.
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Paragraph 0048; 0049
(2016/10/08)
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- 4-Dodecylbenzenesulfonic acid (DBSA) promoted solvent-free diversity-oriented synthesis of primary carbamates, S-thiocarbamates and ureas
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A simple and highly efficient solvent-free method for the conversion of alcohols, phenols, thiols and amines to primary carbamates, S-thiocarbamates and ureas in the presence of 4-dodecylbenzenesulfonic acid (DBSA) as a cheap and green Bronsted acid reagent has been described. All products were obtained in good to excellent yields and characterized using FT-IR, 1H- and 13C-NMR, MS and CHNS techniques.
- Sardarian, Ali Reza,Inaloo, Iman Dindarloo
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p. 76626 - 76641
(2015/09/22)
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- Synthesis of diethylcarbonate by ethanolysis of urea catalysed by heterogeneous mixed oxides
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New Zn- and Ca-based mixed oxides have been tested in the ethanolysis of urea. Cerium and magnesium have revealed to be able to stabilize and enhance the activity of Zn and Ca. All the used compounds act as heterogeneous catalysts in a batch reactor and can be easily recovered and re-used in several catalytic runs. However, although ZnO dissolves as Zn(NCO)2(NH3)2 in the reaction medium under the operative conditions and then partly precipitates at room temperature ensuring a modest immediate recoverability and recyclability, 2CaO/CeO2 is insoluble also at the reaction temperature that makes it well suited even for the use in a flow reactor. MgO-ZnO and SiO2-ZnO have also been tested. The former has an interesting performance, but still not equal to that of 2CaO-CeO2. Interestingly, the latter catalyst is able to convert urea and ethanol into DEC with 91% conversion of urea and 98% selectivity in the long term.
- Angelini,Dibenedetto,Curulla-Ferré,Aresta
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p. 88401 - 88408
(2015/11/03)
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- Catalytic alcoholysis of urea to diethyl carbonate over calcined Mg-Zn-Al hydrotalcite
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The synthesis of diethyl carbonate (DEC) from urea and ethanol was carried out over Mg-Zn-Al composite oxide catalysts derived from hydrotalcites (HTs). The catalytic results showed that the ternary hydrotalcites calcined at 450 °C with Mg:Zn:Al = 1:1.7:1 exhibited superior catalytic activity, and the highest DEC yield was 67.8%. Similar to ethanol, other alcohols such as methanol and butanol can also be transformed to corresponding dialkyl carbonates. Catalysts were characterized by XRD, BET, SEM and TPD with the aim of establishing a relationship between performance and structure. The results indicated that MgZn1.7Al-450 with nanoplate morphology and more accessible active medium basic sites were favourable for obtaining much superior catalytic activity. Recycling experiments demonstrated that the catalyst could be successfully reused. This journal is
- Wang, Peixue,Liu, Shimin,Zhou, Feng,Yang, Benqun,Alshammari, Ahmad S.,Deng, Youquan
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p. 19534 - 19540
(2015/06/15)
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- Unexpectedly Stable (Chlorocarbonyl)(N-ethoxycarbonylcarbamoyl)disulfane, and Related Compounds That Model the Zumach-Weiss-Kühle (ZWK) Reaction for Synthesis of 1,2,4-Dithiazolidine-3,5-diones
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The Zumach-Weiss-Kühle (ZWK) reaction provides 1,2,4-dithiazolidine-3,5-diones [dithiasuccinoyl (Dts)-amines] by the rapid reaction of O-ethyl thiocarbamates plus (chlorocarbonyl)sulfenyl chloride, with ethyl chloride and hydrogen chloride being formed as coproducts, and carbamoyl chlorides or isocyanates generated as yield-diminishing byproducts. However, when the ZWK reaction is applied with (N-ethoxythiocarbonyl)urethane as the starting material, heterocyclization to the putative "Dts-urethane"? does not occur. Instead, the reaction directly provides (chlorocarbonyl)(N-ethoxycarbonylcarbamoyl)disulfane, a reasonably stable crystalline compound; modified conditions stop at the (chlorocarbonyl)[1-ethoxy-(N-ethoxycarbonyl)formimidoyl]disulfane intermediate. The title (chlorocarbonyl)(carbamoyl)disulfane cannot be converted to the elusive Dts derivative, but rather gives (N-ethoxycarbonyl)carbamoyl chloride upon thermolysis, or (N-ethoxycarbonyl)isocyanate upon treatment with tertiary amines. Additional transformations of these compounds have been discovered, providing entries to both known and novel species. X-ray crystallographic structures are reported for the title (chlorocarbonyl)(carbamoyl)disulfane; for (methoxycarbonyl)(N-ethoxycarbonylcarbamoyl)disulfane, which is the corresponding adduct after quenching in methanol; for [1-ethoxy-(N-ethoxycarbonyl)formimidoyl](N′-methyl-N′-phenylcarbamoyl)disulfane, which is obtained by trapping the title intermediate with N-methylaniline; and for (N-ethoxycarbonylcarbamoyl)(N′-methyl-N′-phenylcarbamoyl)disulfane, which is a short-lived intermediate in the reaction of the title (chlorocarbonyl)(carbamoyl)disulfane with excess N-methylaniline. The new chemistry and structural information reported herein is expected to contribute to accurate modeling of the ZWK reaction trajectory.
- Barany, George,Britton, Doyle,Chen, Lin,Hammer, Robert P.,Henley, Matthew J.,Schrader, Alex M.,Young, Victor G.
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p. 11313 - 11321
(2015/12/01)
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- HYDROXY-TERMINATED SILOXANE, POLYSILOXANE-POLYCARBONATE COPOLYMER, AND PREPARATION METHOD THEREOF
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Provided are a hydroxy-terminated siloxane, a polysiloxane-polycarbonate copolymer including same as a repeating unit, and a preparation method thereof. The hydroxyl-terminated siloxane has the structure of chemical formula 1.
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- CATALYST FOR THE SYNTHESIS OF ALKYL CARBAMATES, THE METHOD FOR PREPARING THE SAME AND THE USE THEREOF
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The present invention pertains to a catalyst for the synthesis of organic alkyl carbamates, the method for preparing the same and the use thereof. The catalyst comprises a catalytically active component and a catalyst support, and the catalytically active component being carried by the catalyst support, wherein the catalytically active component comprises a transition metal oxide, and the general formula of the transition metal oxide is EOx, wherein E is selected from transition metal element and x is in the range of 0.5-4.
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Page/Page column 4-5
(2011/07/08)
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- Study of the reaction between carbamoyl azides of α-N-protected amino acids and hydrazine monohydrate
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Two simple and efficient synthetic methods for the preparation of semicarbazide amino acid derivatives are reported. The procedures involve reaction between the carbamoyl azides of α-N-protected amino acids and hydrazine monohydrate: 4-[(alkoxycarbonylamino)(alkyl)methyl]semicarbazides 1 are obtained when hydrazine is added to the separated tetrahydrofuran (THF) solution containing the carbamoyl azide at 0 °C, whereas 1-[(alkoxycarbonylamino)(alkyl)methyl-carbamoyl]-4-[(alkoxycarbonylamino)(alkyl) methyl]semicarbazides 4 are produced by adding hydrazine directly into the final THF/aqueous buffer (KH2PO4) biphasic mixture containing the prepared carbamoyl azide at 50 °C, respectively. NMR experimental data obtained from samples dissolved in [D6]dimethyl sulfoxide suggest a dimeric association for semicarbazides 4 with intermolecular hydrogen bonds. Moreover, the ESI-MS-MS spectra reveal some interesting common features.
- Verardo, Giancarlo,Venneri, Cesare Daniele,Esposito, Gennaro,Strazzolini, Paolo
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scheme or table
p. 1376 - 1384
(2011/04/17)
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- New attempt for CO2 utilization: One-pot catalytic syntheses of methyl, ethyl and n-butyl carbamates
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The direct production of methyl, ethyl and n-butyl carbamates (MC, EC and BC) from NH3, CO2 and alcohols could efficiently be catalyzed by V2O5, and ca. 11-25% yields with 98% selectivity for alkyl carbamates could be obtained. The catalyst could be recycled six times without obvious decrease in catalytic activity. XRD and XPS analysis showed that in-situ produced (NH4)2V 3O8 was the catalytically active species.
- Li, Jian,Qi, Xiujuan,Wang, Liguo,He, Yude,Deng, Youquan
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experimental part
p. 1224 - 1227
(2012/01/13)
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- ORGANOSILICON COMPOUNDS, PRODUCTION PROCESSES THEREOF, PRESSURE-SENSITIVE ADHESIVE COMPOSITIONS CONTAINING THE ORGANOSILICON COMPOUNDS, SELF-ADHESIVE POLARIZERS AND LIQUID CRYSTAL DISPLAYS
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Organosilicon compounds are represented by the following formula: wherein R is a hydrolyzable group, R′ is an alkyl having 1 to 4 carbon atoms, A is an alkylene having 1 to 6 carbon atoms, X is O or S, Y is —NH— or S, L1 and L2 are C or N, Z and M are —NH—, O or S, R1 to R11 are H, alkyl having 1 to 6 carbon atoms, alkoxy or fluoroalkyl, or amino, m is 1 to 3, and n is 0 to 3. R1 and R2 or R2 and R3 may bonded together. R5 and R6 or R9 and R10 may directly bond together. R4 and R7 or R8 and R11 may form a ring skeleton. Their production processes, pressure-sensitive adhesive compositions, self-adhesive polarizers and LCDs are also disclosed.
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- WATER-EMULSIFIABLE POLYISOCYANATES
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The present invention describes a process for preparing water-emusifiable polyisocyanate.
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- Dibutyltin oxide catalyzed aminolysis of oxalate to carbamate, oxamate and derivatives of imidazolidine trione
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Catalytic aminolysis of oxalates by simple and substituted ureas has been shown to give carbamates, oxamates and derivatives of imidazolidine trione. Various substituted ureas and oxalates were screened to verify the applicability of the protocol. The rol
- Kunde, Lalita B.,Kalyani, Vishwanath S.,Gupte, Sunil P.
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experimental part
p. 402 - 407
(2010/08/06)
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- CATALYST FOR THE SYNTHESIS OF ORGANIC CARBONATES, PROCESS FOR PREPARING THE SAME AND APPLICATION THEREOF
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The present invention relates to a catalyst for the synthesis of organic carbonates, the preparation of the catalyst and the application of this catalyst in the synthesis of organic carbonates from reacting urea and hydroxyl group containing compounds. The catalyst provided in this invention is a calcinate of hydrous salt containing rare earth element at a moderate calcining temperature.
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Page/Page column 3
(2010/12/29)
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- NOVEL PREPOLYMERIZABLE SURFACE ACTIVE MONOMERS WITH BOTH FLUORINE-CONTAINING GROUPS AND HYDROPHILIC GROUPS
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Provided are surface modified contact lenses formed from one or more fumaric- or itaconic-containing prepolymers having reactive functionality that is complimentary to surface modifying polymers.
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- MACROCYCLES AND THEIR USES
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The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of diseases
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- A concise synthesis of (S)-N-ethoxycarbonyl-α-methylvaline
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(Chemical Equation Presented) A practical and efficient protocol for the three-step synthesis of (S)-N-emoxycarbonyl-α-methylvaline 3 is described which utilizes readily available commercial starting materials. The key transformations involve resolution-crystallization of tartrate salt 6 followed by a one-pot procedure for the preparation of 3 which is isolated as the dicyclohexylamine salt in 45% overall yield and in 91-95% ee.
- Kuethe, Jeffrey T.,Gauthier Jr., Donald R.,Beutner, Gregory L.,Yasuda, Nobuyoshi
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p. 7469 - 7472
(2008/02/13)
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- Silica supported perchloric acid (HClO4-SiO2): an efficient reagent for the preparation of primary carbamates under solvent-free conditions
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The synthesis of primary carbamates from structurally diverse compounds containing a hydroxyl group has been performed in high yields and purity, and without any epimerization under solvent-free conditions using HClO4-SiO2 as a mild, convenient, and effective reagent. The procedure is operationally simple, efficient, and environmentally benign.
- Modarresi-Alam, Ali Reza,Khamooshi, Ferydoon,Nasrollahzadeh, Mahmoud,Amirazizi, Homeyra Alsadat
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p. 8723 - 8726
(2008/02/11)
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- Cosmetic product, nanoparticles for cosmetics, and powder for cosmetics
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The invention provides a cosmetic product which has a good texture and allows full expression of the inherent functions of ceramide as an intercellular lipid, such as skin barrier function and hair protection effect, as well as nanoparticles for cosmetics and powder for cosmetics which may be used in the above cosmetic product, exhibit good skin barrier function and hair protection effect, and are easy to incorporate into the above cosmetic product. The cosmetic product, the nanoparticles, and the powder for cosmetics according to the present invention contain a polymer obtained by polymerization of a monomer material containing a glycerol (meth)acrylate monomer represented by the formula (1): (R1: -H, -CH3; R2: -(CH2)n-; n is an integer of 1 to 4) .
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- Deodorant and deodorizing article
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A deodorant includes a powder of an amine salt of a phosphorus inorganic acid, the powder having an average particle diameter of 0.1 to 30 μm. The amine salt of a phosphorus inorganic acid is preferably an ammonium salt. Deodorant products including the d
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- Polyether polyol composition and use thereof
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To provide a polyether polyol composition, whereby the reaction rate with a polyisocyanate can be controlled, and an isocyanate group-terminated prepolymer excellent particularly in storage stability can be given. A polyether polyol composition comprising
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- USE OF (R)-PENCICLOVIR TRIPHOSPHATE FOR THE MANUFACTURE OF A MEDICAMENT FOR THE TREATMENT OF VIRAL DISEASES
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A method of treatment of: i) HIV-1 infections in mammals, including humans; or ii) HBV infections in mammals, including humans; which method comprises the administration to the human in need of such treatment, an effective amount of the (R)-enantiomer of the triphosphate of a compound of formula (A) or a pharmaceutically acceptable salt thereof; and compounds for use in the method.
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- 8-aza-bicyclo[3.2.1]octane NMDA/NR2B antagonists
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Novel 3-substituted 8-aza-bicyclo[3.2.1]octanes (commonly known as “tropanes”) substituted in the 8-position are effective as NMDA NR2B antagonists useful for relieving pain.
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- Beta-Amino-Acid derivatives as inhibitors of matrix metalloproteases and TNF-Alpha
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The present application describes novel β-amino acid derivatives of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, X, Z, Ua, Xa, Ya, Za, R1, R2, R3, R4, and R4a are defined in the present specification, which are useful as metalloprotease and/or as TNF-α inhibitors.
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- A simple synthetic protocol for the protection of amides, lactams, ureas, and carbamates
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A new procedure for protecting the amide, lactam, urea, and carbamate NH group with a triphenylmethyl (Tr) group is described. The utility of this method is illustrated with molecules that contain other functional groups. A mild deprotection using trifluoroacetic acid makes this a useful method for attaching amide groups on resin for combinatorial synthesis.
- Reddy, Dandu R,Iqbal, Mohamed A,Hudkins, Robert L,Messina-McLaughlin, Patricia A,Mallamo, John P
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p. 8063 - 8066
(2007/10/03)
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- NOVEL OPIATE COMPOUNDS, METHODS OF MAKING AND METHODS OF USE
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The present application relates to novel opioid receptor antagonists and agonists, methods of making these compounds, and methods of use thereof.
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- Zwitterionic-fatty acid compounds having anti-inflammatory properties
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A composition and method for treating both superficial and subdermal inflammation is taught by treating an inflamed skin area, muscle, or bone joint, with a therapeutically effective amount of a skin-compatible ester of a zwitterionic aminosulphonic acid
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- 4-Aryl-1-(indanmethyl, dihydrobenzofuranmethyl or dihydrobenzothiophene-methyl) piperazines
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4-Aryl-1-(indanmethyl, dihydrobenzofuramethyl or dihydrobenzothiophenemethyl) piperidine, -tetrahydropyridine or -piperazine compounds of general formula (I) wherein one of X and Y is CH2, and the other one is CH2, O or S; Z is N, C, CH or COH; Ar is an optionally substituted aryl group; R1is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, acyl, thioacyl, alkylsulfonyl, trifluoromethylsulfonyl, arylsulfonyl, a group R9VCO— where V is O or S and R9is alkyl or aryl, or a group R10R11NCO— or R10R11NCS— wherein R10and R11are hydrogen, alkyl or aryl, or R10and R11are linked to form a ring; R2is hydrogen, alkyl, cycloalkyl or cycloalkylalkyl; or R1and R2are linked to form a ring; R3-R5are hydrogen, halogen, alkyl, alkylcarbonyl, phenylcarbonyl, alkoxy, alkylthio, hydroxy, alkylsulfonyl, cyano, trifluoromethyl, cycloalkyl, cycloalkylalkyl or nitro; R6and R7are hydrogen or alkyl or they are linked to constitute a 3-7-membered ring; R8is hydrogen or alkyl; have effects at central serotonergic receptors and are therefore useful in the treatment of certain psychic and neurologic disorders.
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- Water dispersible polyisocyanates containing alkoxysilane groups
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The present invention relates to compounds having an isocyanate group content (calculated as NCO, MW 42) of 0.2 to 20% by weight and an alkoxysilane group content (calculated as Si, MW 28) of 0.2 to 4.5% by weight, wherein the preceding percentages are th
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- Multicomponent complex for use with substrate
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Compositions and methods for use with substrates which are useful in the sustained delivery of bioeffecting agents are described. The compositions of the invention include a multicomponent complex which attaches a bioeffecting agent to a substrate with an
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- Process for producing 2,4-oxazolidinedione
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Provided is a process which comprises reacting a 2-hydroxycarboxylic acid ester with urea to form a 2,4-oxazolidinedione , separating an unreacted 2-hydroxycarboxylic acid ester and a catalyst from the resulting reaction solution through distillation, and purifying the fraction composed mainly of the 2,4-oxazolidinedione through crystallization and/or extraction. In accordance with the present invention, the purified 2,4-oxazolidinedione is easily produced in a high yield by a simple purification method without using a costly alkali metal compound.
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- Efficient synthesis of a 1,4-dihydro2H-3,1-benzoxazin-2-one
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An efficient method for the preparation of a compound of (-)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl- 1,4-dihydro-2H-3, 1-benzoxazin-2-one, also known as DMP-266, a reverse transcriptase inhibitor is achieved using a cyclization reaction of the amino alcohol intermediate with an alkyl or aryl chloroformate and a base.
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- Preparation of hydroxy urethanes
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The reactions of cyclic carbonates, especially 1,3-dioxolan-2-ones, with amines, especially primary amines, are catalyzed by the presence of a base whose conjugate acid has a pKa of about 11 or more. The products are hydroxy urethanes, and the process can
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- TACHYKININ ANTAGONISTS
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The invention concerns tachykinin antagonists. The compounds are nonpeptides which have utility in treating disorders mediated by tachykinins. Such disorders are respiratory, inflammatory, gastrointestinal, ophthalmic, allergies, pain, vascular, diseases of the central nervous system, and migraine. Methods of preparing compounds and novel intermediates are also included.The compounds are expected to be especially useful in asthma and rheumatoid arthritis.
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- PIPERIDINE AND HEXAHYDROPYRIDAZINE THROMBIN INHIBITORS
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Compounds of the invention have the following structure: STR1
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- Pancratistatins and processes for their production
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Disclosed are novel pancratistatins and methods for their total asymmetric synthesis. In particular embodiments, processes for the total asymmetric synthesis of (+)-pancratistatin, (-)-pancratistatin, (+)-7-deoxypancratistatin, (-)-7-deoxypancratistatin, truncated pancratistatins, and related derivatives are provided.
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- Aryl substituted heterocycles
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The present invention concerns the novel use of aryl substituted heterocycles of formula I, set out below, which antagonize the pharmacological actions of one of ent endogenous neuropeptide tachykinins an the neurokinin 2 (NK2) receptor making them useful whenever such antagonism is desired, such as in the treatment of asthma and related conditions. The invention also provides pharmaceutical compositions containing the aryl substituted heterocycles for use in such treatment. Certain novel aryl substituted heterocycles of formula I and novel intermediates for their manufacture are also provided. STR1
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- o-Hydroxyphenyl-s-triazines
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o-Hydroxyphenyl-s-triazines are described which contain at least two alkoxyphenyl substituents. They have the formula (1). The compounds according to the invention are suitable as stabilizers for textile fiber materials, in particular polyester fiber materials, and for organic polymers. Furthermore, they are suitable for use as sunscreens in cosmetic preparations.
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- N-substituted cycloalkyl and polycycloalkyl α-substituted Trp-Phe- and phenethylamine derivatives
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Novel unnatural dipeptoids of α-substituted Trp-Phe derivatives useful as agents in the treatment of obesity, hypersecretion of gastric acid in the gut, gastrin-dependent tumors, colorectal tumors, or as antipsychotics are disclosed. Further the compounds are antianxiety agents, antiulcer agents, antidepressant agents, and are agents useful for preventing the withdrawal response produced by chronic treatment or use followed by chronic treatment followed by withdrawal from nicotine, diazepam, alcohol, cocaine, caffeine, or opiods. Also disclosed are pharmaceutical compositions and methods of treatment using the dipeptoids as well as processes for preparing them and novel intermediates useful in their preparation. An additional feature of the invention is the use of the subject compounds to prepare pharmaceutical and diagnostic compositions.
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