专利号:US-10844088-B2 优先权日:2011-07-19 标 题:Process for the preparation of estetrol 发明人:PLATTEEUW JOHANNES JAN; COELINGH BENNINK HERMAN JAN TIJMEN; DAMEN FRANCISCUS WILHELMUS PETRUS; VAN VLIET MICHIEL CHRISTIAN ALEXANDER 权利人:DONESTA BIOSCIENCE B V; ESTETRA SPRL 摘要:The present invention relates to a process for the preparation of estra-1,3,5(10)-trien-3, 15a, 16a, 17β-tetraol (estetr-01), via a silyl enol ether derivative 17-B-oxy-3-A-oxy-estra-1,3,5(10), 16-tetraene, wherein A is a protecting group and B is —Si(R 2 ) 3 . The invention further relates to a process for the synthesis of 3-A-oxy-estra-1,3,5(10), 15-tetraen-17-one, in which A is a protecting group, via silyl enol ether derivative 17-B-oxy-3-A-oxy-estra-1,3,5(10),16-tetraene, and B is —Si(R 2 ) 3 .
专利号:US-5670666-A 优先权日:1993-09-27 标题:Process for preparing intermediates for the synthesis of D1 antagonists 发明人:HOU DONALD; DRAPER RICHARD W; LEE GARY M; MAS JANET L 权利人:SCHERING CORP 摘要:Disclosed are a process and intermediates of the formulae ##STR1## wherein X - is halide, BF 4 - , R 3 SO 3 - , wherein R 3 is C 1 -C 6 alkyl, CF 3 , C 1 -C 6 alkylphenyl or phenyl, and Q is a group of the formula ##STR2## wherein R is C 1 -C 6 alkyl; useful for preparing benzazepine intermediates of the formula ##STR3## These benzazepine intermediates are useful for preparing benzazepines having activity as selective D1 receptor antagonists.
专利号:US-6943194-B1 优先权日:1998-01-09 标题:Synthesis of phenstatin and prodrugs thereof 发明人:PETTIT GEORGE R; TOKI BRIAN 权利人:UNIV ARIZONA STATE 摘要:A newly discovered antineoplastic compound denominated “phenstatinâ€? is herein described as are synthetic methods for producing phenstatin and the active prodrug thereof. Phenstatin was converted to the sodium phosphate prodrug (3d) by a dibenzylphosphite phosphorylation and subsequent hydrogenolysis sequence 3b→3c→3d. Phenstatin (3b) was found to be a potent inhibitor of tubulin polymerization and the binding of colchicine to tubulin comparable to combretastatin A-4 (1b).
专利号:US-7220870-B2 优先权日:1995-03-14 标 题:Hydrolytic kinetic resolution of cyclic substrates 发明人:JACOBSEN ERIC N; TOKUNAGA MAKOTO; LARROW JAY F 权利人:HARVARD COLLEGE 摘要:The present invention relates to a process for stereoselective or regioselective chemical synthesis which generally comprises reacting a nucleophile and a chiral or prochiral cyclic substrate in the presence of a non-racemic, chiral catalyst to produce a stereoisomerically- and/or regioisomerically-enriched product. The present invention also relates to hydrolytic kinetic resolutions of racemic and diastereomeric mixtures of epoxides.
专利号:US-2024287010-A1 优先权日:2021-06-23 标题:Process For Making Epoxide Derivatives of Farnesene and Use Thereof in Further Synthesis 发明人:PERSIANI GIACOMO; BAUMGARTNER CORINNE; GRANIER THIERRY; LOVCHIK MARTIN; SCHROEDER FRIDTJOF 权利人:GIVAUDAN SA 摘要:Described herein are methods for making intermediates in the production of fragrance ingredients starting from β-farnesene. In particular, methods for making acetylmethylfarnesol and hydroxy-farnesylacetone are described. Methods for making other intermediates in the process are also described. In addition, compositions comprising intermediates in the process and uses of the intermediates are described.
专利号:WO-9509156-A1 优先权日:1993-09-27 标 题 :Processes and intermediates for the enantiospecific synthesis of benzo(d)naphth(2.1-b)azepines