CN109496215A - 一种福沙匹坦磷酸酯中间体及其制备方法 - Google Patents

一种福沙匹坦磷酸酯中间体及其制备方法 Download PDF

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Publication number
CN109496215A
CN109496215A CN201780021165.9A CN201780021165A CN109496215A CN 109496215 A CN109496215 A CN 109496215A CN 201780021165 A CN201780021165 A CN 201780021165A CN 109496215 A CN109496215 A CN 109496215A
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fosaprepitant
methods according
item
alkali
phosphate intermediate
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CN201780021165.9A
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CN109496215B (zh
Inventor
张继承
栗增
黄鲁宁
陈茜
陶安平
顾虹
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Shanghai Aobo Biomedical Co ltd
Zhejiang Huahai Pharmaceutical Co Ltd
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Zhejiang Huahai Pharmaceutical Co Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65583—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C213/00—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
    • C07C213/08—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions not involving the formation of amino groups, hydroxy groups or etherified or esterified hydroxy groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • C07C215/02—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C215/04—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated
    • C07C215/06—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic
    • C07C215/10—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic with one amino group and at least two hydroxy groups bound to the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biochemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

提供一种福沙匹坦磷酸酯中间体(IV)的制备方法、福沙匹坦磷酸酯中间体(IV‑A)以及使用中间体(IV‑A)制备福沙匹坦二甲葡胺的方法(AA)，IV：R1、R2独立地选自C1‑C7烷基或苄基；IV‑A：R1、R2独立地选自C1‑C7烷基或苄基，并且R1、R2不同时为苄基

Description

PCT国内申请，说明书已公开。

Claims (22)

  1. PCT国内申请，权利要求书已公开。
CN201780021165.9A 2016-05-09 2017-05-09 一种福沙匹坦磷酸酯中间体及其制备方法 Active CN109496215B (zh)

Applications Claiming Priority (3)

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CN2016103008907 2016-05-09
CN201610300890.7A CN107353303B (zh) 2016-05-09 2016-05-09 一种福沙匹坦磷酸酯中间体的制备方法
PCT/CN2017/083630 WO2017193913A1 (zh) 2016-05-09 2017-05-09 一种福沙匹坦磷酸酯中间体及其制备方法

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CN109496215A true CN109496215A (zh) 2019-03-19
CN109496215B CN109496215B (zh) 2021-07-23

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US (1) US11091508B2 (zh)
EP (1) EP3456726B1 (zh)
CN (2) CN107353303B (zh)
WO (1) WO2017193913A1 (zh)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113045605B (zh) * 2021-03-30 2022-06-07 浙江亚瑟医药有限公司 一种福沙匹坦二甲葡胺的制备方法和纯化方法

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010018595A2 (en) * 2008-07-17 2010-02-18 Glenmark Generics Limited Fosaprepitant dimeglumine intermediate, neutral fosaprepitant, and amorphous fosaprepitant dimeglumine and processes for their preparations
WO2011163594A2 (en) * 2010-06-24 2011-12-29 Alkermes, Inc. Prodrugs of nh-acidic compounds: ester, carbonate, carbamate and phosphonate derivatives
WO2013168176A2 (en) * 2012-03-30 2013-11-14 Glenmark Generics Limited Process for preparation of fosaprepitant and salt thereof
CN104098604A (zh) * 2013-04-10 2014-10-15 山东省生物药物研究院 一种制备福沙匹坦二甲葡胺的方法
CN104650142A (zh) * 2013-11-25 2015-05-27 山东新时代药业有限公司 一种福沙匹坦二甲葡胺的制备方法
CN106432337A (zh) * 2015-08-08 2017-02-22 陕西合成药业股份有限公司 福沙匹坦衍生物、合成和在长效制剂中的用途

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW385308B (en) 1994-03-04 2000-03-21 Merck & Co Inc Prodrugs of morpholine tachykinin receptor antagonists
WO2011045817A2 (en) 2009-10-15 2011-04-21 Sandoz Private Limited Process for the preparation of fosaprepitant, intermediate and pharmaceutical acceptable salt thereof

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010018595A2 (en) * 2008-07-17 2010-02-18 Glenmark Generics Limited Fosaprepitant dimeglumine intermediate, neutral fosaprepitant, and amorphous fosaprepitant dimeglumine and processes for their preparations
WO2011163594A2 (en) * 2010-06-24 2011-12-29 Alkermes, Inc. Prodrugs of nh-acidic compounds: ester, carbonate, carbamate and phosphonate derivatives
US9072788B2 (en) * 2010-06-24 2015-07-07 Alkermes Pharma Ireland Limited Prodrugs of NH-acidic compounds: ester, carbonate, carbamate and phosphonate derivatives
WO2013168176A2 (en) * 2012-03-30 2013-11-14 Glenmark Generics Limited Process for preparation of fosaprepitant and salt thereof
CN104098604A (zh) * 2013-04-10 2014-10-15 山东省生物药物研究院 一种制备福沙匹坦二甲葡胺的方法
CN104650142A (zh) * 2013-11-25 2015-05-27 山东新时代药业有限公司 一种福沙匹坦二甲葡胺的制备方法
CN106432337A (zh) * 2015-08-08 2017-02-22 陕西合成药业股份有限公司 福沙匹坦衍生物、合成和在长效制剂中的用途

Also Published As

Publication number Publication date
EP3456726B1 (en) 2020-12-02
US20190144477A1 (en) 2019-05-16
CN109496215B (zh) 2021-07-23
CN107353303B (zh) 2020-09-01
CN107353303A (zh) 2017-11-17
EP3456726A4 (en) 2019-12-11
EP3456726A1 (en) 2019-03-20
US11091508B2 (en) 2021-08-17
WO2017193913A1 (zh) 2017-11-16

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Address after: 317024 Flood Bridge, Linhai City, Taizhou City, Zhejiang Province

Patentee after: ZHEJIANG HUAHAI PHARMACEUTICAL Co.,Ltd.

Patentee after: Shanghai Aobo biomedical Co.,Ltd.

Address before: 317024 Flood Bridge, Linhai City, Taizhou City, Zhejiang Province

Patentee before: ZHEJIANG HUAHAI PHARMACEUTICAL Co.,Ltd.

Patentee before: SHANGHAI AOBO PHARMTECH, Inc.,Ltd.

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