CAS: 119141-88-7; (S)-6-Methoxy-2-(((4-Methoxy-3,5-Dimethylpyridin-2-yl)Methyl)Sulfinyl)-1H-Benzo[d]Imidazole

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CAS号73590-85-9 奥美拉唑硫醚 | CAS号21286-54-4 (1S)-(+)-樟脑－10－磺酰氯 | CAS号73590-58-6 奥美拉唑 | CAS号1080503-75-8 (-)-menthyl (S)... | CAS号109371-19-9 4-甲氧基-2,3,5-三甲基吡啶

奥美拉唑置于escherichia Coli Dmso Reductase体系中,用 甲醇,Aq. Phosphate Buffer 用作溶剂,化学反应 3.0H,以98%的收率获得
参考文献:手性亚砜的酶动力学拆分-对映体互补方法†
标题:手性亚砜的酶动力学拆分-对映体互补方法†
摘要:描述了一种新的用于制备手性亚砜的酶促测定方法,该方法与甲硫氨酸亚砜还原酶a(msra)的已知的(S)-对映异构体还原活性是对映体互补的.为此,我们利用了dmso还原酶(dmsabc),该酶最近被我们发现在固定相大肠杆菌中高度上调.
Doi:10.1039/c9Cc05470G

专利信息

专利号:WO-9002605-A1
优先权日:1988-09-02
标题:An apparatus and a method for the synthesis of peptides
发明人：MELDAL MORTEN; HOLM ARNE; BUCHARDT OLE
权利人:MELDAL MORTEN; HOLM ARNE; BUCHARDT OLE
摘要:An apparatus for use in chemical synthesis, especially peptide synthesis, comprises a synthesis chamber unit having a multiplicity of synthesis chambers, each of which has a liquid inlet and a liquid outlet, means for introducing liquid into the individual synthesis chambers and means for simultaneous removal of liquid via the liquid outlets of the synthesis chambers by regulation of the fluid pressure difference between the liquid inlets and the liquid outlets. A method for peptide synthesis using such an apparatus comprises the provision in each of the synthesis chambers of a solid-phase support material having a first, at least N-protected amino acid coupled thereto, after which a liquid deprotection reagent is introduced into the synthesis chambers. Following deprotection, the deprotection reagent is removed, after which a second, at least N-protected amino acid is introduced into each synthesis chamber in order to couple the first and second amino acids. Third, fourth, etc. amino acids may be coupled analogously. Complete removal of the deprotection reagent from the synthesis chambers and the support material can be ensured by incorporating a stable, intensely coloured dye, e.g., azorubin, in the deprotection reagent. The apparatus and the method make possible the parallel synthesis of a large number of peptides, e.g. peptides having overlapping amino acid sequences and constituting part of a longer peptide chain. The apparatus can be adapted to manual, semi-automatic or fully automatic performance of the various steps in the synthesis procedure.

专利号:US-8173817-B2
优先权日:2004-05-28
标 题 :Stereoselective synthesis of benzimidazole sulfoxides
发明人：REDDY BANDI PARTHASARADHI; REDDY KURA RATHNAKAR; REDDY RAPOLU RAJI; REDDY DASARI MURALIDHARA
权利人:REDDY BANDI PARTHASARADHI; REDDY KURA RATHNAKAR; REDDY RAPOLU RAJI; REDDY DASARI MURALIDHARA; HETERO DRUGS LTD
摘要:The present invention relates to a process for stereoselective synthesis of substituted sulfoxides either as a single enantiomer or in an enantiomerically enriched form. Thus, 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]thio]-1H-benzimidazole is reacted with (R)-camphorsulfonyl chloride to form a mixture of 1-(R)-camphorsulfonyl-5- (and 6-)methoxy-2-[(3,5-dimethyl-4-methoxy-2-pyridyl)methylthio]-1H-benzimidazole, oxidized to obtain a diastereomeric excess of 1-(R)-camphorsulfonyl-(5- and 6-)-methoxy-2-[(3,5-dimethyl-4-methoxy-2-pyridyl)methyl-(S)-sulfinyl]-1H-benzimidazole over 1-(R)-camphorsulfonyl-(5- and 6-)-methoxy-2-[(3,5-dimethyl-4-methoxy-2-pyridyl)methyl-(R)-sulfinyl]-1H-benzimidazole, the diastereomers are separated by fractional crystallization and the separated 1-(R)-camphorsulfonyl-(5- and 6-)-methoxy-2-[(3,5-dimethyl-4-methoxy-2-pyridyl)methyl-(S)-sulfinyl]-1H-benzimidazole is deprotected to give esomeprazole.

专利号:US-7211590-B2
优先权日:2002-08-01
标 题:Nitrosated proton pump inhibitors, compositions and methods of use
发明人：FANG XINQIN; GARVEY DAVID S; LETTS L GORDON
权利人:NITROMED INC
摘要:The invention describes novel nitrosated proton pump inhibitor compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated proton pump inhibitor compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one nitrosated proton pump inhibitor compound, and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one nitrosated proton pump inhibitor compound, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating gastrointestinal disorders; facilitating ulcer healing; decreasing the recurrence of ulcers; improving gastroprotective properties, anti-Helicobacter pylori properties or antacid properties of proton pump inhibitors; decreasing or reducing the gastrointestinal toxicity associated with the use of nonsteroidal antiinflammatory compounds; treating bacterial infections and/or viral infections.

专利号:US-9981949-B2
优先权日:2008-12-01
标题 :Synthesis and novel salt forms of (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine
发明人：AKIREDDY SRINIVASA RAO; BHATTI BALWINDER SINGH; CUTHBERTSON TIMOTHY J; DULL GARY MAURICE; MILLER CRAIG HARRISON; MITCHENER JR JOSEPH PIKE; MUNOZ JULIO A; OTTEN PIETER ALBERT
权利人:OYSTER POINT PHARMA INC
摘要:The present invention relates to the stereospecific synthesis of (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine, its salt forms, and novel polymorphic forms of these salts.

专利号:US-2008287407-A1
优先权日:2003-12-10
标题 :Nitric Oxide Releasing Pyruvate Compounds, Compositions and Methods of Use
发明人：GARVEY DAVID S; FANG XINQIN; KHANAPURE SUBHASH P; RANATUNGA RAMANI R; WEY SHIOW-JYI
权利人:NITROMED INC
摘要:The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one pyruvate compound and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one pyruvate compound, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating diseases resulting from oxidative stress, diabetes, reperfusion injury following ischemia, preservation of tissues, organs, organ parts and/or limbs.

专利号:US-8304409-B2
优先权日:2002-07-03
标 题:Nitrosated nonsteroidal antiinflammatory compounds, compositions and methods of use
发明人：EARL RICHARD A; EZAWA MAIKO; FANG XINQIN; GARVEY DAVID S; GASTON RICKY D; KHANAPURE SUBHASH P; LETTS L GORDON; LIN CHIA-EN; RANATUNGE RAMANI R; RICHARDSON STEWART K; SCHROEDER JOSEPH D; STEVENSON CHERI A; WEY SHIOW-JYI
权利人:EARL RICHARD A; EZAWA MAIKO; FANG XINQIN; GARVEY DAVID S; GASTON RICKY D; KHANAPURE SUBHASH P; LETTS L GORDON; LIN CHIA-EN; RANATUNGE RAMANI R; RICHARDSON STEWART K; SCHROEDER JOSEPH D; STEVENSON CHERI A; WEY SHIOW-JYI; NICOX SA
摘要:The invention describes novel nitrosated nonsteroidal antiinflammatory drugs (NSAIDs) and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated NSAID, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one nitrosated NSAID, and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one nitrosated NSAID, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating inflammation, pain and fever; for treating gastrointestinal disorders; for facilitating wound healing; for treating and/or preventing gastrointestinal, renal and/or respiratory toxicities resulting from the use of nonsteroidal antiinflammatory compounds; for treating inflammatory disease states and/or disorders; and for treating and/or preventing ophthalmic diseases and/or disorders.