CAS: 103577-45-3; 2-(((3-Methyl-4-(2,2,2-Trifluoroethoxy)Pyridin-2-yl)Methyl)Sulfinyl)-1H-Benzo[d]Imidazole

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CAS号666727-70-4 2-[[[3-Methyl-4... | CAS号103577-40-8 兰索拉唑硫醚 | CAS号163119-30-0 兰索拉唑硫醚-N-氧化物 | CAS号408332-88-7 D-(-)-tartaric ... | CAS号344268-32-2 dibutyl D-tartrate | CAS号13811-71-7 D-酒石酸二乙酯 | CAS号1116-76-3 三辛胺 | CAS号37699-43-7 2,3-二甲基-4-硝基吡啶-N-氧化物 | CAS号138530-94-6 右旋兰索拉唑 | CAS号138530-95-7 (S)-兰索拉唑

2-[[[3-甲基-4-(2,2,2三氟乙氧基)-2-吡啶]-甲基]硫基]-1H-苯并咪唑置于间氯过氧苯甲酸体系中,化学反应生成兰索拉唑
参考文献:通过新的恶唑烷鎓盐将硫化物高度对映选择性氧化为亚砜.
标题:通过新的恶唑烷鎓盐将硫化物高度对映选择性氧化为亚砜.
摘要:新的恶二氮杂鎓盐5(r2 = Tbdps)是有效的试剂,用于将硫化物高度对映体选择性氧化为亚砜,Ee最高可达99%以上,且收率很高.因此,它代表了现有的不对称硫氧化方法的一种新的有价值的非金属替代品.
Doi:10.1021/ol0702573

专利信息

专利号:US-5948789-A
优先权日:1994-07-15
标题:Process for synthesis of substituted sulphoxides
发明人：LARSSON MAGNUS ERIK; STENHEDE URBAN JAN; SOERENSEN HENRIK; VON UNGE SVERKER PER OSKAR; COTTON HANNA KRISTINA
权利人:ASTRA AB
摘要:PCT No. PCT/SE95/00818 Sec. 371 Date Jul. 14, 1995 Sec. 102(e) Date Jul. 14, 1995 PCT Filed Jul. 3, 1995 PCT Pub. No. WO96/02535 PCT Pub. Date Feb. 1, 1996A novel process for enantioselective synthesis of single enantiomers of omeprazole or its alkaline salts, of other optically pure substituted 2-(2-pyridinylmethyl-sulphinyl) -1H-benzimidazoles as well as of other structurally related sulphoxides or their alkaline salts. The claimed process is an asymmetric oxidation of a pro-chiral sulphide to the single enantiomers or an enantiomerically enriched form of the corresponding sulphoxide. The application also claims the enantiomeric sulphoxide products produced by the process and their use in medicine.

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:WO-02061120-A1
优先权日:2001-02-01
标题:Method of evaluating ability of drug to induce enzyme in liver cells
发明人：OHTA KUNIHIRO; NAKAGAWA TOSHITO
权利人:CHUGAI PHARMACEUTICAL CO LTD; OHTA KUNIHIRO; NAKAGAWA TOSHITO
摘要:A method of evaluating the ability of a test drug to induce the synthesis of CYP (cytochrome P450) in liver cells characterized by comprising culturing the liver cells in a culture medium containing the test drug in the presence of matrigel and evaluating the ability of the test drug to induce the synthesis of CYP by assaying the enzymatic activity of CYP in the culture medium.

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.