CAS: 459789-99-2; (R)-4-((3R,5S,6R,7R,8S,9S,10S,13R,14S,17R)-6-Ethyl-3,7-Dihydroxy-10,13-Dimethylhexadecahydro-1H-Cyclopenta[a]Phenanthren-17-yl)Pentanoic Acid

上下游产品

奥贝胆酸杂质a 3α,7β-Dihydroxy-6α-Ethyl-5β-Cholan-24-Oic Acid 865244-30-0
鹅去氧胆酸 Chenodeoxycholic Acid 474-25-9
去氧胆酸 Deoxycholic Acid 83-44-3
石胆酸 Lithocholic Acid 434-13-9
猪去氧胆酸 Hyodeoxycholic Acid 83-49-8
猪去氧胆酸甲酯 Methyl Hyodeoxycholate 2868-48-6
(5β,6α,7β)-6-Ethyl-7-Hydroxy-3-Oxocholan-24-Oic Acid Ethyl Ester
3α-羟基-7-氧代-5β-胆烷酸 7-Ketolithocholic Acid 4651-67-6
Methyl 3α-7α-Ditrimethylsilyloxy-5β-Chol-6-En-24-Oate 52759-80-5
3α-羟基-7-氧代-胆烷酸-24-甲酯 7-Ketolithocholic Methyl Ester 10538-59-7

3α-羟基-7-氧代-5β-胆烷酸置于potassium Fluoride,Sodium Tetrahydroborate,磷酸,Palladium On Activated Charcoal,三氟化硼,氢气,三氟乙酸,Sodium Hydroxide,Lithium Diisopropyl Amide体系中,用 四氢呋喃,甲醇,二氯甲烷,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 52.0H,反应生成 奥贝胆酸
参考文献:一种3α-羟基-7-氧代-5β-胆烷酸新衍生物制备奥贝胆酸的方法
标题:一种3α-羟基-7-氧代-5β-胆烷酸新衍生物制备奥贝胆酸的方法
摘要:本发明公开了3α‑羟基‑7‑氧代‑5β‑胆烷酸新衍生物制备奥贝胆酸的方法,所述合成方法包括以下步骤:首先将3α‑羟基‑7‑氧代‑5β‑胆烷酸进行羟基和羧基保护制备相应的新衍生物,其次按照两条合成路线分别得到奥贝胆酸.本发明使用更安全的保护基试剂,解决了中间体紫外吸收不强的问题,使得中间体更容易纯化,提高了收率,降低了成本,更适合工业化放大,有显著的创造性和实际应用价值.

专利信息

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-2023114753-A1
优先权日:2020-03-06
标 题 :Use of a group of markers for diagnosing and adjusting treatment of primary biliary cholangitis, pharmaceutical composition and solid dosage form for treating primary biliary cholangitis
发明人：JAIN NITIN
权利人:MILI HEALTHCARE TRADE DMCC LLC
摘要:A method of diagnosis and treatment of primary biliary cholangitis is provided. Additionally, a pharmaceutical composition and a solid dosage form for the treatment of primary biliary cholangitis, containing ursodeoxycholic and obeticholic acids, are provided. The technical contribution resides in obtaining a new all-purpose pharmaceutical composition and solid dosage form for the treatment of PBC, which includes both ursodeoxycholic and obeticholic acids, which is effective in use at all stages of PBC and has a complex mechanism of action. In particular, simultaneous blockage of the transport and synthesis of bile acids is achieved.

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-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-10301350-B2
优先权日:2014-11-19
标题 :6-alkyl-7-hydroxy-4-en-3-one steroids as intermediates for the production of steroidal FXR modulators
发明人：WEYMOUTH-WILSON ALEXANDER; KOMSTA ZOFIA; BOYDELL JAMES; OTTER CARL; WALLIS LAURA; BATCHELOR RHYS
权利人:NZP UK LTD
摘要:The invention relates to compounds of formula (I) and related methods, wherein R 1 , R 2 , Y, R 4 and R 5 are as defined herein. The compounds are intermediates in the synthesis of synthetic bile acids with pharmacological activity. The invention futher provides intermediated in the systhesis of obeticholic acid and its analogues. The invention also provides methods related to the synthesizing of these intermediates and methods of preparing obeticholic acid and obeticholic acid analogues from the compound of the invention.

专利号:US-11104702-B2
优先权日:2017-07-18
标题 :Process and intermediates for the synthesis of obeticholic acid and derivatives thereof
发明人：HERRÃ?IZ SIERRA IGNACIO; FERNÃ?NDEZ SAINZ YOLANDA; CORDOVILLA LOSADA CARLOS; PÉREZ ENCABO ALFONSO; TURIEL HERNANDEZ JOSÉ ANGEL
权利人:CRYSTAL PHARMA SAU
摘要:A process for the preparation of obeticholic acid and derivatives thereof by:(a) hydrogenation of the double bond and reductive opening of the epoxide of a compound of formula (II) or a salt or solvate thereofto obtain a compound of formula (IIIa) and/or (IIIb), or salts or solvates thereofand(b) conversion of a compound of formula (IIIa) and/or a compound of formula (IIIb), or a salt or solvate thereof, into a compound of formula (I), or a salt or solvate thereof