CAS: 4651-67-6; 7-Ketolithocholic Acid

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10538-59-7 68170-81-0 1632118-78-5

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CAS号474-25-9 鹅去氧胆酸； 鹅脱氧胆酸 | CAS号2646-38-0 鹅去氧胆酸钠 | CAS号434-13-9 石胆酸 | CAS号1448-36-8 胆酸甲酯 | CAS号3057-04-3 鹅脱氧胆酸甲酯 | CAS号186649-59-2 (3R,5R,7R,8R,9S... | CAS号151112-03-7 (3R,5R,7R,8R,9S... | CAS号186649-58-1 (3R,5S,7R,8R,9S... | CAS号547-75-1 猪胆酸 | CAS号474-25-9 鹅去氧胆酸； 鹅脱氧胆酸 | CAS号83-49-8 猪去氧胆酸 | CAS号10538-55-3 熊去氧胆酸甲酯

胆酸置于吡啶,Chromium(Vi) Oxide,7α-Hydroxysteroid Dehydrogenase,Nicotinamide Adenine Dinucleotide Phosphate体系中,化学反应生成 3α-羟基-7-氧代-5β-胆烷酸
参考文献:P450 单加氧酶的工程区域选择性能够通过石胆酸的 7β-羟基化合成熊去氧胆酸
标题:P450 单加氧酶的工程区域选择性能够通过石胆酸的 7β-羟基化合成熊去氧胆酸
摘要:我们从抗生素链霉菌中改造了细胞色素 P450 单加氧酶 Cyp107D1 (Olep),用于石胆酸 (Lca) 的立体和区域选择性 7β-羟基化,产生熊去氧胆酸 (Udca).此前研究表明,Olep 可在 7β 位羟基化睾酮,但 Lca 仅在 6β 位羟基化,形成鼠脱氧胆酸 (Mdca).使用结构和 3Dm 分析以及分子对接来鉴定氨基酸残基 F84,S240 和 V291 作为特异性决定残基.丙氨酸扫描鉴定出 S240A 是产生 Udca 的变体.使用 Udca 比色测定法筛选基于这些位置的合成"小而智能"文库.我们鉴定了一种几乎完美的区域和立体选择性三重突变体(f84Q/s240A/v291G),其产生的 Udca 水平比 S240A 变体高 10 倍.这种生物催化剂为从生物废品 Lca 中环保合成 Udca 开辟了新的可能性.
DOI:10.1002/anie.202012675

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-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:WO-2021214685-A1
优先权日:2020-04-21
标 题:Method for the synthesis of a cholane derivative
发明人：GALDI GIANLUCA; SACCO PAOLO; PIATEK ANNA MARIA; VESTRI ALESSANDRO
权利人:BAR PHARMACEUTICALS SOC A RESPONSABILITA LIMITATA
摘要:The present invention refers to a method for the preparation of a compound of formula (I).

专利号:US-10544441-B2
优先权日:2014-06-24
标 题 :Method for biocatalytic whole cell reduction of dehydrocholic acid compounds, and 7-β-hydroxysteroid dehydrogenase mutants
发明人：WEUSTER-BOTZ DIRK; SUN BOQIAO; QUIRIN CHRISTIAN
权利人:PHARMAZELL GMBH
摘要:The invention relates to novel biocatalytic processes comprising the whole cell reduction of dehydrocholic acid (DHCA) compounds, novel 7β-hydroxy steroid dehydrogenase mutants, the sequences coding for these enzyme mutants, methods for producing the enzyme mutants and use thereof in enzymatic conversions of cholic acid compounds, and in particular in the production of ursodesoxycholic acid (UDCA); also a subject of the invention are novel methods for the synthesis of UDCA using the enzyme mutants; and in particular a further improved method for producing UDCA using recombinant whole cell biocatalysts.