专利号:US-7452994-B2 优先权日:2001-09-12 标 题 :Synthesis of enantiomerically pure amino-substituted fused bicyclic rings 发明人:MCEACHERN ERNEST J; BRIDGER GARY J; SKUPINSKA KRYSTYNA A; SKERLJ RENATO T; YANG WEN 权利人:ANORMED INC 摘要:This invention describes various processes for synthesis and resolution of racemic amino-substituted fused bicyclic ring systems. One process utilizes selective hydrogenation of an amino-substituted fused bicyclic aromatic ring system. An alternative process prepares the racemic amino-substituted fused bicyclic ring system via nitrosation. In addition, the present invention describes the enzymatic resolution of a racemic mixture to produce the (R)- and (S)-forms of amino-substituted fused bicyclic rings as well as a racemization process to recycle the unpreferred enantioner. Further provided by this invention is an asymmetric synthesis of the (R)- or (S)-enantiomer of primary amino-substituted fused bicyclic ring systems.
专利号:US-8084630-B2 优先权日:2007-05-31 标 题 :Process for the synthesis of ramelteon and its intermediates 发明人:KANSAL VINOD KUMAR; MISTRY DHIRENKUMAR N; VASOYA SANJAY L; RAFILOVICH MICHAL; MOHA-LERMAN ELENA BEN; LIFSHITZ-LIRON REVITAL 权利人:KANSAL VINOD KUMAR; MISTRY DHIRENKUMAR N; VASOYA SANJAY L; RAFILOVICH MICHAL; MOHA-LERMAN ELENA BEN; LIFSHITZ-LIRON REVITAL; TEVA PHARMA 摘要:The present invention provides processes and intermediates for the synthesis of ramelteon.
专利号:US-2009281176-A1 优先权日:2007-11-01 标题:Process for the synthesis of ramelteon and its intermediates 发明人:KANSAL VINOD KUMAR; MISTRY DHIRENKUMAR N; VASOYA SANJAY L; PATEL RAKESH; JADAV ARPAN M 权利人:KANSAL VINOD KUMAR; MISTRY DHIRENKUMAR N; VASOYA SANJAY L; PATEL RAKESH; JADAV ARPAN M 摘要:A process for the preparation of ramelteon and intermediates useful in the process. The process suitable for industrial scale provides increased yield and/or greater purity with fewer process steps.
专利号:US-5300437-A 优先权日:1989-06-22 标 题 :Enantiomeric enrichment and stereoselective synthesis of chiral amines 发明人:STIRLING DAVID I; MATCHAM GEORGE W; ZEITLIN ANDREW L 权利人:CELGENE CORP 摘要:Amines in which the amino group is on a secondary carbon atom which is chirally substituted can be enantiomerically enriched by the action of an omega-amino acid transaminase which has the property of preferentially converting one of the two chiral forms to a ketone. The process also can be used to stereoselectively synthesize one chiral form from ketones substantially to the exclusion of the other.
专利号:US-5169780-A 优先权日:1989-06-22 标题:Enantiomeric enrichment and stereoselective synthesis of chiral amines 发明人:STIRLING DAVID I; ZEITLIN ANDREW L; MATCHAM GEORGE W; ROZZELL JR JAMES D 权利人:CELGENE CORP 摘要:Amines in which the amino group is on a secondary carbon atom which is chirally substituted can be enantiomerically enriched by the action of an omega-amino acid transaminase which has the property of preferentially converting one of the two chiral forms to a ketone. The process can be used to stereoselectively sythesize one chiral form from ketones substantially to the exclusion of the other. An aqueous solution of chiral amines after being brought into contact with an omega-amino acid transaminase and an amino acceptor is treated with a water-immiscible organic solvent, the aqueous and organic phases are separated, and the aqueous phase can be recirculated for further contact with the transaminase.
专利号:US-8487094-B2 优先权日:2008-07-25 标题 :Synthesis of inhibitors of 11β-hydroxysteroid dehydrogenase type 1 发明人:FANDRICK KEITH R; GAO JOE JU; LI WENJIE; LU ZHI-HUI; ZHANG YONGDA 权利人:FANDRICK KEITH R; GAO JOE JU; LI WENJIE; LU ZHI-HUI; ZHANG YONGDA; BOEHRINGER INGELHEIM INT 摘要:Disclosed are syntheses of 11β-HSD1 inhibitors and corresponding intermediates that are promising for the treatment of a variety of disease states including diabetes, metabolic syndrome, obesity, glucose intolerance, insulin resistance, hyperglycemia, hypertension, hypertension-related cardiovascular disorders, hyperlipidemia, deleterious gluco-corticoid effects on neuronal function (e.g. cognitive impairment, dementia, and/or depression), elevated intra-ocular pressure, various forms of bone disease (e.g., osteoporosis), tuberculosis, leprosy (Hansen's disease), psoriasis, and impaired wound healing (e.g., in patients that exhibit impaired glucose tolerance and/or type 2 diabetes).