WO2023138341A9 - 一种厄他培南钠的合成方法 - Google Patents

一种厄他培南钠的合成方法 Download PDF

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Publication number
WO2023138341A9
WO2023138341A9 PCT/CN2022/143602 CN2022143602W WO2023138341A9 WO 2023138341 A9 WO2023138341 A9 WO 2023138341A9 CN 2022143602 W CN2022143602 W CN 2022143602W WO 2023138341 A9 WO2023138341 A9 WO 2023138341A9
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WO
WIPO (PCT)
Prior art keywords
synthesis method
ertapenem sodium
ertapenem
present application
sodium
Prior art date
Application number
PCT/CN2022/143602
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English (en)
French (fr)
Other versions
WO2023138341A1 (zh
Inventor
姜能江
林楠棋
欧军
王东
幸志伟
孙万鹏
Original Assignee
深圳市海滨制药有限公司
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
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Publication date
Application filed by 深圳市海滨制药有限公司 filed Critical 深圳市海滨制药有限公司
Publication of WO2023138341A1 publication Critical patent/WO2023138341A1/zh
Publication of WO2023138341A9 publication Critical patent/WO2023138341A9/zh

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D477/00—Heterocyclic compounds containing 1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbapenicillins, thienamycins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulphur-containing hetero ring
    • C07D477/02—Preparation
    • C07D477/06—Preparation from compounds already containing the ring or condensed ring systems, e.g. by dehydrogenation of the ring, by introduction, elimination or modification of substituents
    • C07D477/08—Modification of a carboxyl group directly attached in position 2, e.g. esterification
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D477/00—Heterocyclic compounds containing 1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbapenicillins, thienamycins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulphur-containing hetero ring
    • C07D477/10—Heterocyclic compounds containing 1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbapenicillins, thienamycins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulphur-containing hetero ring with hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 4, and with a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, e.g. an ester or nitrile radical, directly attached in position 2
    • C07D477/12—Heterocyclic compounds containing 1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbapenicillins, thienamycins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulphur-containing hetero ring with hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 4, and with a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, e.g. an ester or nitrile radical, directly attached in position 2 with hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached in position 6
    • C07D477/16—Heterocyclic compounds containing 1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbapenicillins, thienamycins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulphur-containing hetero ring with hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 4, and with a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, e.g. an ester or nitrile radical, directly attached in position 2 with hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached in position 6 with hetero atoms or carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. an ester or nitrile radical, directly attached in position 3
    • C07D477/20—Sulfur atoms

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Molecular Biology (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Catalysts (AREA)

Abstract

本申请属于药物合成技术领域，尤其涉及一种厄他培南钠的合成方法。本申请提供了一种厄他培南钠的合成方法，包括以下步骤：在碱、催化剂和氢气气氛的条件下，将式1所示化合物与混合溶剂混合进行氢化反应，过滤得到产物溶液，乙酸乙酯萃取提纯，水相调节pH值至4～7，得到酸性产物溶液；于所述酸性产物溶液中加入析晶溶剂进行析晶，得到厄他培南钠；所述厄他培南钠具有式2所示结构。本申请提供了一种厄他培南钠的合成方法，有效解决现有厄他培南合成方法中存在的需要进行繁琐的后处理，产能小，产品重金属残留高，纯度差的技术问题。
PCT/CN2022/143602 2022-01-24 2022-12-29 一种厄他培南钠的合成方法 WO2023138341A1 (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN202210076557.8A CN114105988B (zh) 2022-01-24 2022-01-24 一种厄他培南钠的合成方法
CN202210076557.8 2022-01-24

Publications (2)

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WO2023138341A1 WO2023138341A1 (zh) 2023-07-27
WO2023138341A9 true WO2023138341A9 (zh) 2023-09-14

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WO (1) WO2023138341A1 (zh)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114105988B (zh) * 2022-01-24 2022-04-29 深圳市海滨制药有限公司 一种厄他培南钠的合成方法

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1060180B1 (en) * 1998-03-02 2006-03-29 Merck & Co., Inc. Process for synthesizing carbapenem antibiotics
WO2012038979A2 (en) * 2010-09-24 2012-03-29 Sequent Anti Biotics Private Limited A process for preparation of ertapenem
CN102731506B (zh) * 2011-04-13 2015-08-12 石药集团中奇制药技术（石家庄）有限公司 一种厄他培南及其钠盐的制备方法
CN102690266B (zh) * 2011-09-02 2014-06-18 深圳市海滨制药有限公司 一种制备厄他培南钠的方法
WO2013121279A2 (en) * 2012-02-14 2013-08-22 Aurobindo Pharma Limited Process to prepare ertapenem
WO2015087245A1 (en) * 2013-12-11 2015-06-18 Unimark Remedies Ltd. Process for preparation of ertapenem and salts thereof
CN106279175A (zh) * 2016-08-12 2017-01-04 上海龙翔生物医药开发有限公司 一种厄他培南单钠盐的制备方法
CN114105988B (zh) * 2022-01-24 2022-04-29 深圳市海滨制药有限公司 一种厄他培南钠的合成方法

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CN114105988A (zh) 2022-03-01
WO2023138341A1 (zh) 2023-07-27
CN114105988B (zh) 2022-04-29

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