📜二去甲胆烯醛置于硫酸体系中,用 乙醇,水 用作溶剂,化学反应 0.33H,反应生成20-甲酰基孕甾-4-烯-3-酮 参考文献:Synthesis Of Methyl (20R,22E)-And (20S,22E)-3-Oxochola-1,4,22-Trien-24-Oate 标题:Synthesis Of Methyl (20R,22E)-And (20S,22E)-3-Oxochola-1,4,22-Trien-24-Oate 摘要:Methyl (22E)-3-Oxochola-1,4,22-Trien-24-Oate (4; C25H34O3) Is A Naturally occurring Steroid With Unknown Configuration At C(20). Starting From The (20S)-3-Oxo-23,24-Dinorchol-4-En-22-Al (1A),We Prepared Both Diastereoisomeric Methyl Esters 4A And 4B By A Three-Step Procedure (Scheme). In The Case Of 4B,The Initial Epimerization Of Aldehyde La Was Followed By Completion Of The Sequence And Then Separation Via Fractional Crystallization To Afford Pure (20R)-Methyl Ester 4A And Its (20S)-Diastereomer 4B. Only The Analytical Data Of The (20S)-Compound 4B Were In Good Agreement With Those Reported For The Natural Product. Doi:10.1002/1522-2675(200204)85:4<1096::Aid-Hlca1096>3.0.Co;2-U
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-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:EP-0734392-B1 优先权日:1993-12-17 标题:Conversion of bisnoralcohol to bisnoraldehyde 发明人:HEWITT BRADLEY DEE 权利人:UPJOHN CO 摘要:The present invention is a process for the conversion of bisnoralcohol (I) to bisnoraldehyde (II) which is a known intermediate in the synthesis of progesterone.
专利号:US-6133280-A 优先权日:1997-02-05 标题 :Androgen synthesis inhibitors 发明人:BRODIE ANGELA; LING YANGZHI 权利人:UNIV MARYLAND 摘要:This invention relates to novel inhibitors of androgen synthesis that are useful in the treatment of prostate cancer and benign prostatic hypertrophy. The present invention also provides methods of synthesizing these novel compounds, pharmaceutical compositions containing these novel compounds, and methods of treating prostate cancer and benign prostatic hypertrophy using the androgen synthesis inhibitors of the present invention.
专利号:US-2019284227-A1 优先权日:2016-05-18 标题:Intermediates for the Synthesis of Bile Acid Derivatives, in Particular of Obeticholic Acid
专利号:WO-2017199033-A1 优先权日:2016-05-18 标题:Intermediates for the synthesis of bile acid derivatives, in particular of obeticholic acid
参考标题:Synthesis Of C-C Bonded Dimeric Steroids By Olefin Metathesis 作者:Valeria C. Edelsztein,Pablo H. Di Chenna,Gerardo Burton |发布日期:2009.5 摘要:Five New C-C Bonded Steroidal Homodimers Derived From Deoxycholic Acid, Pregnenolone, And Progesterone Were Synthesized By An Olefin Metathesis Reaction Assisted By Microwave Heating. Microwave Improved The Yield And Accelerated The Reaction Allowing The Use Of Less Catalyst With Good Results (2.5 Mol %). Due To The Bulky Nature Of The Steroidal Skeleton The More Favorable E-Dimers Were Formed As The
合成参考文献
摘要:Lin, S.; Yan, L.; Liu, P., Science of Synthesis, (2007) 20, 97. 摘要:Yan, L.; Lin, S.; Liu, P., Science of Synthesis, (2007) 20, 741. 摘要:Sammakia, T.; Abramite, J. A.; Sammons, M. F., Science of Synthesis, (2007) 33, 408.