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3α-羟基-7-氧代-5β-胆烷酸置于对甲苯磺酸体系中,用 甲醇 用作溶剂,以95%的收率获得3α-羟基-7-氧代-胆烷酸-24-甲酯
参考文献:一种奥贝胆酸及中间体的合成方法
标题:一种奥贝胆酸及中间体的合成方法
摘要:本发明公开了一种奥贝胆酸及中间体的合成方法,具体涉及以鹅去氧胆酸,Nbs,浓硫酸,甲醇,碘化钠,三甲基氯化硅,三乙胺,乙醛,三氟化硼乙醚,钯碳和氢气,Naoh,Nabh4为原料,经过氧化反应,酯化反应,保护反应,Aldol反应,氢化还原,水解,羰基还原反应七步反应,本发明提供的一种奥贝胆酸及中间体的合成方法是一种高收率,低成本,环保,易操作,适宜工业化的合成方法.

专利信息

专利号:US-9982008-B2
优先权日:2012-06-19
标题 :Preparation and uses of obeticholic acid
发明人：STEINER ANDRÉ; WAENERLUND POULSEN HEIDI; JOLIBOIS EMILIE; REWOLINSKI MELISSA; GROSS RALF; SHARP EMMA; DUBAS-FISHER FIONA; EBERLIN ALEX
权利人:INTERCEPT PHARMACEUTICALS INC
摘要:The present invention relates to obeticholic acid: n nor a pharmaceutically acceptable salt, solvate or amino acid conjugate thereof. Obeticholic acid is useful for the treatment or prevention of a FXR mediated disease or condition, cardiovascular disease or cholestatic liver disease, and for reducing HDL cholesterol, for lowering triglycerides in a mammal, or for inhibition of fibrosis. The present invention also relates to processes for the synthesis of obeticholic acid.

专利号:US-9732116-B2
优先权日:2012-06-19
标 题 :Preparation and uses of obeticholic acid
发明人：STEINER ANDRÉ; WAENERLUND POULSEN HEIDI; JOLIBOIS EMILIE; REWOLINSKI MELISSA; GROSS RALF; SHARP EMMA; DUBAS-FISHER FIONA; EBERLIN ALEX
权利人:INTERCEPT PHARMACEUTICALS INC
摘要:The present invention relates to obeticholic acid: n nor a pharmaceutically acceptable salt, solvate or amino acid conjugate thereof. Obeticholic acid is useful for the treatment or prevention of a FXR mediated disease or condition, cardiovascular disease or cholestatic liver disease, and for reducing HDL cholesterol, for lowering triglycerides in a mammal, or for inhibition of fibrosis. The present invention also relates to processes for the synthesis of obeticholic acid.

专利号:US-4962099-A
优先权日:1988-01-11
标 题:Chemical synthesis
发明人：MOSBACH ERWIN H; MCSHERRY CHARLES K; UNE MIZUHO; MATOBA NAOYUKI
权利人:BETH ISRAEL MEDICAL CENTER
摘要:A process for the production of disubstituted bile acid analogs, including the disubstituted analogs of such bile acids as, lithocholic, hyodeoxycholic, cholic, chenodeoxycholic and ursodeoxycholic acids. n This invention was made in the course of work performed under a grant from the U.S. National Heart Lung and Blood Institute.

专利号:CN-115819491-A
优先权日:2022-12-22
标题 :Synthesis method of 7-ketolithocholic acid and ursodeoxycholic acid