CN112424211A - 一种曲氟尿苷的制备方法 - Google Patents

一种曲氟尿苷的制备方法 Download PDF

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Publication number
CN112424211A
CN112424211A CN201980047151.3A CN201980047151A CN112424211A CN 112424211 A CN112424211 A CN 112424211A CN 201980047151 A CN201980047151 A CN 201980047151A CN 112424211 A CN112424211 A CN 112424211A
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China
Prior art keywords
compound
formula
solvent
formula iii
mass
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CN201980047151.3A
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CN112424211B (zh
Inventor
刘林
赵瑞
桑光明
周兴健
郭晓鹏
张爱明
吴刚
夏春光
张喜全
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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
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H1/00—Processes for the preparation of sugar derivatives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06—Pyrimidine radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06—Pyrimidine radicals
    • C07H19/073—Pyrimidine radicals with 2-deoxyribosyl as the saccharide radical
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • General Health & Medical Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

本申请涉及曲氟尿苷的制备方法，包括式III化合物和式IV化合物在酸存在下，在第一溶剂中反应得到式II化合物，并进一步反应得到曲氟尿苷。

Description

PCT国内申请，说明书已公开。

Claims (14)

  1. PCT国内申请，权利要求书已公开。
CN201980047151.3A 2018-07-24 2019-07-24 一种曲氟尿苷的制备方法 Active CN112424211B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201810817373 2018-07-24
CN2018108173736 2018-07-24
PCT/CN2019/097439 WO2020020208A1 (zh) 2018-07-24 2019-07-24 一种曲氟尿苷的制备方法

Publications (2)

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CN112424211A true CN112424211A (zh) 2021-02-26
CN112424211B CN112424211B (zh) 2021-12-24

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CN201980047151.3A Active CN112424211B (zh) 2018-07-24 2019-07-24 一种曲氟尿苷的制备方法

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US (1) US11702439B2 (zh)
EP (1) EP3828192B1 (zh)
CN (1) CN112424211B (zh)
AU (1) AU2019310704B2 (zh)
CA (1) CA3106057A1 (zh)
WO (1) WO2020020208A1 (zh)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112362791B (zh) * 2020-12-10 2023-06-06 国药一心制药有限公司 一种曲氟尿苷与其异构体的hplc分离方法

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5006646A (en) * 1989-02-22 1991-04-09 Yuki Gosei Kogyo Co., Ltd. Process for preparing 2'-deoxy-5-trifluoromethyl-beta-uridine
CN103130855A (zh) * 2011-11-30 2013-06-05 连云港润众制药有限公司 一种地西他滨的制备方法
CN105461772A (zh) * 2015-11-23 2016-04-06 国药一心制药有限公司 一种曲氟尿苷中间体及曲氟尿苷的制备方法
CN106220699A (zh) * 2016-07-21 2016-12-14 嘉实（湖南）医药科技有限公司 高纯度曲氟尿苷的制备方法
CN109021048A (zh) * 2018-08-13 2018-12-18 江苏悦兴医药技术有限公司 一种曲氟尿苷工艺杂质的合成方法
WO2019049174A1 (en) * 2017-09-07 2019-03-14 Msn Laboratories Private Limited, R&D Center SOLID STATE FORMS OF 5-CHLORO-6 - [(2-IMINOPYRROLIDIN-1-YL) METHYL] PYRIMIDINE-2,4- (1H, 3H) -DIONE HYDROCHLORIDE AND METHODS OF PREPARATION THEREOF

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE60114098T2 (de) * 2000-02-10 2006-05-18 Mitsui Chemicals, Inc. Ein Verfahren zur Herstellung von Trifluorothymidinderivaten
CN100334100C (zh) * 2004-01-17 2007-08-29 杭州富邦生物制药有限公司 5－三氟甲基－2’－脱氧尿苷的合成方法

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5006646A (en) * 1989-02-22 1991-04-09 Yuki Gosei Kogyo Co., Ltd. Process for preparing 2'-deoxy-5-trifluoromethyl-beta-uridine
CN103130855A (zh) * 2011-11-30 2013-06-05 连云港润众制药有限公司 一种地西他滨的制备方法
CN105461772A (zh) * 2015-11-23 2016-04-06 国药一心制药有限公司 一种曲氟尿苷中间体及曲氟尿苷的制备方法
CN106220699A (zh) * 2016-07-21 2016-12-14 嘉实（湖南）医药科技有限公司 高纯度曲氟尿苷的制备方法
WO2019049174A1 (en) * 2017-09-07 2019-03-14 Msn Laboratories Private Limited, R&D Center SOLID STATE FORMS OF 5-CHLORO-6 - [(2-IMINOPYRROLIDIN-1-YL) METHYL] PYRIMIDINE-2,4- (1H, 3H) -DIONE HYDROCHLORIDE AND METHODS OF PREPARATION THEREOF
CN109021048A (zh) * 2018-08-13 2018-12-18 江苏悦兴医药技术有限公司 一种曲氟尿苷工艺杂质的合成方法

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
RYAN, KENNETH J. ET AL.: "Chemical synthesis of 2"-deoxy-5-(trifluoromethyl)uridine and theα-D anomer", 《JOURNAL OF ORGANIC CHEMISTRY》 *

Also Published As

Publication number Publication date
US20210292356A1 (en) 2021-09-23
EP3828192A4 (en) 2022-04-20
WO2020020208A1 (zh) 2020-01-30
AU2019310704A1 (en) 2021-03-11
US11702439B2 (en) 2023-07-18
CA3106057A1 (en) 2020-01-30
EP3828192B1 (en) 2023-12-13
AU2019310704B2 (en) 2022-05-19
EP3828192A1 (en) 2021-06-02
CN112424211B (zh) 2021-12-24

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