专利号:US-5606041-A 优先权日:1992-06-26 标题:Process for steroidal peracyl glycosides 发明人:BUSCH FRANK R; GOGGIN KATHLEEN D; LAMBERT JOHN F; SHINE RUSSELL J; WALINSKY STANLEY W 权利人:PFIZER 摘要:Processes for the synthesis of tigogenin beta-O-cellobioside heptaalkanoate which is an intermediate for the known hypo-cholesterolemic agent tigogenin beta-cellobioside. The process comprises reacting α-cellobiosyl bromide heptaalkanoate and β-tigogenin in the presence of zinc fluoride or zinc cyanide under conditions capable of forming said tigogenyl β-O-cellobioside heptaalkanoate. The analogous preparations of hecogenin β-O-cellobioside heptaalkanoate 11-ketotigogenin β-O-cellobioside heptaalkanoate, and diosgenin β-O-cellobioside heptaalkanoate are also disclosed. The process provides both high β-anomeric selectivity and high yields.
专利号:US-5530107-A 优先权日:1992-10-15 标 题:Method for making steroidal peracyl glycosides 发明人:ALLAN DOUGLAS J M; BUSCH FRANK R; LAMBERT JOHN F; SHINE RUSSELL J; WALINSKY STANLEY W 权利人:PFIZER 摘要:Processes for the synthesis of tigogenin beta-O-cellobioside heptaalkanoate which is an intermediate for the known hypocholesterolemic agent tigogenin beta-cellobioside. The process comprises reacting α-cellobiosyl bromide heptaalkanoate and β-tigogenin in the presence of zinc fluoride or zinc cyanide under conditions capable of forming said tigogenyl β-O-cellobioside heptaalkanoate. The analogous preparations of hecogenin β-O-cellobioside heptaalkanoate, 11-ketotigogenin β-O-cellobioside heptaalkanoate, and diosgenin β-O-cellobioside heptaalkanoate are also disclosed. The process provides both high β-anomeric selectivity and high yields.
专利号:US-5563259-A 优先权日:1992-06-26 标 题:Process for making β-O-cellobiosyl steroid derivatives and trimethyl silyl steroid intermediates used therein 发明人:GOGGIN KATHLEEN D; LAMBERT JOHN F; WALINSKY STANLEY W 权利人:PFIZER 摘要:A process for the synthesis of peracyl-1-O-steroidal-β-cellobiosides that provides excellent β-anomeric selectivity without the use of a metal salt promoter. The process comprises reacting heptaacyl-β-D-cellobiosyl-1-fluoride and a trisubstituted silyl-3-O-steroid, wherein the steroid is tigogenin, hecogenin, 11-ketotigogenin or diosgenin in the absence of a metal salt under suitable conditions.
专利号:US-5010185-A 优先权日:1989-06-13 标 题:Processes for tigogenin beta-cellobioside 发明人:URBAN FRANK J 权利人:PFIZER 摘要:Improved processes for the synthesis of tigogenin beta-cellobioside, a known hypocholesterolemic agent, using cellobiose heptaacetate and tigogenin as starting materials.
专利号:US-8722864-B2 优先权日:2010-07-22 标 题 :Glycosylated acetaminophen pro-drug analogs 发明人:SHULL BRIAN; BALDWIN JOHN; GOPALASWAMY RAMESH; HAROON ZISHAN 权利人:SHULL BRIAN; BALDWIN JOHN; GOPALASWAMY RAMESH; HAROON ZISHAN; NUTEK PHARMA LTD 摘要:The present invention relates to methods and compositions for the synthesis, production, and use of pro-drug analogs of the analgesic acetaminophen. This invention relates to a method for the production of a broad group of glycosides of acetaminophen derivatives.
专利号:US-5294703-A 优先权日:1992-05-01 标 题:Process for preparing α-D-cellobiose octaacetate 发明人:HYATT JOHN A; SANDER TONY L; NAYLOR D MARK; BERNARD BOBBY L 权利人:EASTMAN KODAK CO 摘要:Provided is a novel improved process for the preparation of α-D-cellobiose octaacetate via the acetylative degradation of cellulose or cellulose acetate. The title compound is provided in high yield and quality in a facile one-pot process, amenable to large-scale synthesis.