专利号:US-8236976-B2 优先权日:2004-03-09 标 题 :Processes for highly enantio- and diastereoselective synthesis of acyclic epoxy alcohols and allylic epoxy alcohols 发明人:WALSH PATRICK; LURAIN ALICE E; KELLY ANN R; MAESTRI AARON G 权利人:WALSH PATRICK; LURAIN ALICE E; KELLY ANN R; MAESTRI AARON G; UNIV PENNSYLVANIA 摘要:The inventive subject matter relates to novel processes for making an epoxy alcohol from an aldehyde, comprising the steps of: (a) adding (i) an organozinc compound or (ii) divinylzinc compound and an diorganozinc compound to said aldehyde in the presence of a first catalyst to form an allylic alkoxide compound; and (b) epoxidizing said allylic alkoxide compound in the presence of an oxidant and a second catalyst.
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).
专利号:WO-2007039492-A1 优先权日:2005-09-26 标 题:Efficient synthesis of asymmetric epoxidation catalyst i 发明人:VIDAL I FERRAN ANTON; NIETO ALONSO NATALIA; MOLA PORQUERAS PINEDA 权利人:INST CATALA D INVESTIGACIO QUI; ICREA; VIDAL I FERRAN ANTON; NIETO ALONSO NATALIA; MOLA PORQUERAS PINEDA 摘要:A process for the preparation of chiral ketone I from diol II comprising the acetylation of diol II with an acetylating agent, preferably an acetic acid derivative, wherein said acetylation is performed in the presence of a Lewis acid. The process can further comprise additional previous steps, so that chiral ketone I can be prepared in four steps starting from D-fructose. Alternatively, a process for the preparation of chiral ketone V from diol VI comprising the acetylation of diol VI with an acetylating agent, preferably an acetic acid derivative, wherein said acetylation is performed in the presence of a Lewis acid. The process can further comprise additional previous steps, so that chiral ketone V can be prepared starting from L-fructose, L-sorbose or D-arabinose.
专利号:US-2010256363-A1 优先权日:2007-07-26 标题 :SYNTHESIS OF INHIBITORS OF 11ß-HYDROXYSTEROID DEHYDROGENASE TYPE 1
专利号:US-2011269957-A1 优先权日:2008-07-25 标 题 :Synthesis of inhibitors of 11beta-hydroxysteroid dehydrogenase type 1
专利号:US-2009163728-A1 优先权日:2004-03-09 标题 :Processes for Highly Enantio- and Diastereoselective Synthesis of Acyclic Epoxy Alcohols and Allylic Epoxy Alcohols
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