专利号:US-11479577-B2 优先权日:2016-05-18 标题:Intermediates for the synthesis of bile acid derivatives, in particular of obeticholic acid 发明人:WEYMOUTH-WILSON ALEXANDER; KOMSTA ZOFIA; WALLIS LAURA; EVANS TIMOTHY; DAVIES IEUAN; OTTER CARL; BATCHELOR RHYS 权利人:NZP UK LTD 摘要:The present invention relates to compounds which are intermediates in the synthesis of bile acid derivatives with pharmacological activity. The invention relates to compounds of general formula (I):wherein:, R1, R2, R3, R4, R5, R6 and Y are as defined herein.The compounds are intermediates in the synthesis of synthetic bile acids which are useful in the treatment of conditions such as liver disease. In addition, the invention relates to a method of synthesizing these intermediates and a method of preparing obeticholic acid and obeticholic acid analogues from the compounds of the invention.
专利号:US-6271379-B1 优先权日:2000-03-08 标题:Intermediates useful for the synthesis of huperzine A 发明人:TUECKMANTEL WERNER; KOZIKOWSKI ALAN P 权利人:UNIV GEORGETOWN 摘要:Intermediates useful for the synthesis of huperzine A represented by the structures below, n and methods for their synthesis, wherein: n R 1 is lower alkyl, benzyl, or substituted benzyl; n X is a suitable leaving group; n Y is an electron withdrawing group that can subsequently be converted into an amino group; n one broken line is present as a carbon—carbon bond and the other broken line is absent, where the broken line forms an unconjugated carbon—carbon double bond, which double bond may be endocyclic whereby n is 3 or the double bond may be exocyclic whereby n is 2.
专利号:US-10766921-B2 优先权日:2016-05-18 标 题 :Process and intermediates for the 6,7-alpha-epoxidation of steroid 4,6-dienes 发明人:WEYMOUTH-WILSON ALEXANDER; KOMSTA ZOFIA; WALLIS LAURA; EVANS TIMOTHY 权利人:NZP UK LTD 摘要:The invention relates to a process for preparing a compound of general formula (Ia): wherein R2, Y, R4 and R5 are as defined herein, wherein the epoxidation is conducted using an oxidant and methyltrioxorhenium as a catalyst (MeReO3). The invention also relates to certain compounds per se. The compounds are intermediates in the synthesis of synthetic bile acids.
专利号:US-5688933-A 优先权日:1989-10-16 标题 :Preparation of biologically active compounds from substantially pure enantiomers of 2-azabicyclo 2.2.1!hept-5-en-one 发明人:EVANS CHRISTOPHER THOMAS; ROBERTS STANLEY MICAHEL 权利人:CHIROSCIENCE LTD 摘要:Lactams of 1-amino-3-carboxylic acid cyclic compounds are provided in enantiomeric form, together with an enantiomer of the corresponding ring-opened amino-acid or ester, by reaction of the racemic lactam with a novel lactamase. The products are useful in the synthesis of chiral carbocyclic nucleotides. The enantiomer is preferably 2-azabicyclo 2.2.1!hept-5-en-3-one.
专利号:US-5284769-A 优先权日:1989-10-16 标题 :Process for preparing a single enantiomer of a lactam using lactamase 发明人:EVANS CHRISTOPHER T; ROBERTS STANLEY M 权利人:CHIROS LTD 摘要:Lactams of 1-amino-3-carboxylic acid cyclic compounds are produced in enantiomeric form, together with an enantiomer of the corresponding ring-opened amino-acid or ester, by reaction of the racemic lactam with a novel lactamase. The products are useful in the synthesis of chiral carbocyclic nucleotides.
专利号:WO-2007093765-A1 优先权日:2006-02-13 标题 :Process for the cyanation of aldehydes 发明人:NORTH MICHAEL; BELOKON YURI 权利人:NPIL PHARMACEUTICALS UK LTD; NORTH MICHAEL; BELOKON YURI 摘要:The present invention relates to a process for the cyanation of aldehydes, particularly to the asymmetric cyanation of aldehydes, including the synthesis of chiral cyanohydrins and derivatives thereof, such as chiral O-acyl cyanohydrins. The process of the present invention comprises: reacting the aldehyde with a cyanating agent in the presence of a chiral catalyst and less than a stoichiometric amount of an ionic cyanide source. Chiral catalysts employed in the process according to the present invention are of the formula: (1), (3a), (3b).
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