CN111247160A - 一种胆酸类化合物的制备方法 - Google Patents

一种胆酸类化合物的制备方法 Download PDF

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Publication number
CN111247160A
CN111247160A CN201880069969.0A CN201880069969A CN111247160A CN 111247160 A CN111247160 A CN 111247160A CN 201880069969 A CN201880069969 A CN 201880069969A CN 111247160 A CN111247160 A CN 111247160A
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formula
compound
acid
compound shown
preparation
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CN111247160B (zh
Inventor
张喜全
程兴栋
张爱明
夏春光
陈浪
高策
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Chia Tai Tianqing Pharmaceutical Group Co Ltd
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Chia Tai Tianqing Pharmaceutical Group Co Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J9/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
    • C07J9/005—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane containing a carboxylic function directly attached or attached by a chain containing only carbon atoms to the cyclopenta[a]hydrophenanthrene skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0094—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 containing nitrile radicals, including thiocyanide radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J51/00—Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00

Abstract

本申请属于药物化学领域，涉及一种胆酸类化合物的制备方法。具体而言，本申请提供了一种如式I所示化合物的制备方法，包括使式2化合物发生氧化反应得到式3化合物，式3化合物连接三甲基硅烷基得式4化合物，式4化合物与乙醛反应得式5化合物，式5化合物发生催化氢化反应得式6化合物，式6化合物的氰基转变为羧基得到式I化合物。该制备方法收率高，所需纯化操作少，适合工业化应用。

Description

PCT国内申请，说明书已公开。

Claims (15)

  1. PCT国内申请，权利要求书已公开。
CN201880069969.0A 2017-11-02 2018-11-01 一种胆酸类化合物的制备方法 Active CN111247160B (zh)

Applications Claiming Priority (3)

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CN201711062367 2017-11-02
CN2017110623676 2017-11-02
PCT/CN2018/113326 WO2019085963A1 (zh) 2017-11-02 2018-11-01 一种胆酸类化合物的制备方法

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CN111247160A true CN111247160A (zh) 2020-06-05
CN111247160B CN111247160B (zh) 2021-09-28

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US (1) US11111265B2 (zh)
EP (1) EP3705487B1 (zh)
CN (1) CN111247160B (zh)
WO (1) WO2019085963A1 (zh)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN115611961B (zh) * 2022-10-18 2024-02-13 湖南科瑞生物制药股份有限公司 胆酸中间体a2及其制备方法

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016173524A1 (zh) * 2015-04-29 2016-11-03 正大天晴药业集团股份有限公司 鹅去氧胆酸衍生物
CN106661079A (zh) * 2014-05-29 2017-05-10 巴尔制药有限公司 用于治疗和/或预防fxr和tgr5/gpbar1介导的疾病的胆烷衍生物

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE69940958D1 (de) 1998-12-23 2009-07-16 Glaxo Group Ltd Bestimmungsmethode fur liganden der nuklearen rezeptoren
ITMI20021532A1 (it) * 2002-07-12 2004-01-12 Roberto Pellicciari Composti chimici
AU2013352288B2 (en) * 2012-11-28 2017-11-23 Intercept Pharmaceuticals, Inc. Treatment of pulmonary disease
DK3310801T3 (da) * 2015-06-19 2021-06-21 Intercept Pharmaceuticals Inc Tgr5-modulatorer og fremgangsmåder til anvendelse deraf
MY196292A (en) * 2016-01-28 2023-03-24 Chia Tai Tianqing Pharmaceutical Group Co Ltd Steroid Derivative Fxr Agonist

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106661079A (zh) * 2014-05-29 2017-05-10 巴尔制药有限公司 用于治疗和/或预防fxr和tgr5/gpbar1介导的疾病的胆烷衍生物
WO2016173524A1 (zh) * 2015-04-29 2016-11-03 正大天晴药业集团股份有限公司 鹅去氧胆酸衍生物

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Publication number Publication date
CN111247160B (zh) 2021-09-28
US11111265B2 (en) 2021-09-07
WO2019085963A1 (zh) 2019-05-09
EP3705487B1 (en) 2022-10-26
EP3705487A1 (en) 2020-09-09
US20200347091A1 (en) 2020-11-05
EP3705487A4 (en) 2021-08-04

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