CN102858791A - 制备氟胞苷衍生物的方法 - Google Patents

制备氟胞苷衍生物的方法 Download PDF

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Publication number
CN102858791A
CN102858791A CN2010800325446A CN201080032544A CN102858791A CN 102858791 A CN102858791 A CN 102858791A CN 2010800325446 A CN2010800325446 A CN 2010800325446A CN 201080032544 A CN201080032544 A CN 201080032544A CN 102858791 A CN102858791 A CN 102858791A
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CN
China
Prior art keywords
impurity
compound
formula
capecitabine
area percent
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Pending
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CN2010800325446A
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English (en)
Chinese (zh)
Inventor
胡聪成
黃宏聪
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Scinopharm Taiwan Ltd
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Scinopharm Taiwan Ltd
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Publication of CN102858791A publication Critical patent/CN102858791A/zh
Pending legal-status Critical Current

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    • 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
    • C07H19/067—Pyrimidine radicals with ribosyl as the saccharide radical
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • C07D239/545—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/553—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms with halogen atoms or nitro radicals directly attached to ring carbon atoms, e.g. fluorouracil
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12P—FERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE
    • C12P19/00—Preparation of compounds containing saccharide radicals
    • 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)
  • General Health & Medical Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Molecular Biology (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Microbiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
CN2010800325446A 2009-07-23 2010-07-21 制备氟胞苷衍生物的方法 Pending CN102858791A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US22797109P 2009-07-23 2009-07-23
US61/227,971 2009-07-23
PCT/SG2010/000276 WO2011010967A1 (en) 2009-07-23 2010-07-21 Process for producing flurocytidine derivatives

Publications (1)

Publication Number Publication Date
CN102858791A true CN102858791A (zh) 2013-01-02

Family

ID=43497887

Family Applications (1)

Application Number Title Priority Date Filing Date
CN2010800325446A Pending CN102858791A (zh) 2009-07-23 2010-07-21 制备氟胞苷衍生物的方法

Country Status (8)

Country Link
US (1) US20110021769A1 (https=)
EP (1) EP2456778A4 (https=)
JP (1) JP2012533618A (https=)
KR (1) KR20120037932A (https=)
CN (1) CN102858791A (https=)
AR (1) AR077498A1 (https=)
TW (1) TW201103550A (https=)
WO (1) WO2011010967A1 (https=)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103910773A (zh) * 2014-04-08 2014-07-09 宁波美诺华药业股份有限公司 卡培他滨杂质的合成方法
CN106496294A (zh) * 2016-09-21 2017-03-15 齐鲁天和惠世制药有限公司 一种制备微粉型卡培他滨的方法
CN107936075A (zh) * 2017-12-28 2018-04-20 山东铂源药业有限公司 一种卡培他滨中间体的合成方法
CN109651466A (zh) * 2018-12-20 2019-04-19 深圳市祥根生物科技有限公司 卡培他滨杂质g的制备方法

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103059085B (zh) * 2011-12-27 2015-09-02 石药集团中奇制药技术（石家庄）有限公司 一种抗癌药物中间体及其制备方法
CN103183713B (zh) * 2011-12-31 2015-08-05 沈阳药科大学 5-脱氧-d-呋喃核糖氧苷类化合物的制备方法
CN104628804A (zh) * 2015-01-30 2015-05-20 吉林修正药业新药开发有限公司 一种卡培他滨杂质乙酰缩合物的合成方法
CN121405756A (zh) * 2025-12-29 2026-01-27 赤峰制药股份有限公司 一种卡培他滨中间体的结晶方法

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1033183A (zh) * 1987-11-17 1989-05-31 弗·哈夫曼-拉罗切有限公司 氟胞嘧啶核苷衍生物
CN1094056A (zh) * 1992-12-18 1994-10-26 霍夫曼-拉罗奇有限公司 N-氧羰基取代的5′-脱氧-5-氟胞苷衍生物
CN1095070A (zh) * 1992-12-18 1994-11-16 霍夫曼-拉罗奇有限公司 制备n4-酰基-5′-脱氧-5-氟胞苷衍生物的新方法
CN1935828A (zh) * 2006-10-31 2007-03-28 浙江海正药业股份有限公司 一种含氟嘧啶类化合物烷氧羰酰化的方法
WO2008131062A2 (en) * 2007-04-20 2008-10-30 Dr. Reddy's Laboratories Ltd. Process for preparing capecitabine
WO2008145403A1 (en) * 2007-06-01 2008-12-04 Synthon B.V. Processes related to making capecitabine
WO2009066892A1 (en) * 2007-11-19 2009-05-28 Hanmi Pharm. Co., Ltd. Methods for preparing capecitabine and beta-anomer-rich trialkyl carbonate compound used therein

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1033183A (zh) * 1987-11-17 1989-05-31 弗·哈夫曼-拉罗切有限公司 氟胞嘧啶核苷衍生物
CN1094056A (zh) * 1992-12-18 1994-10-26 霍夫曼-拉罗奇有限公司 N-氧羰基取代的5′-脱氧-5-氟胞苷衍生物
CN1095070A (zh) * 1992-12-18 1994-11-16 霍夫曼-拉罗奇有限公司 制备n4-酰基-5′-脱氧-5-氟胞苷衍生物的新方法
CN1935828A (zh) * 2006-10-31 2007-03-28 浙江海正药业股份有限公司 一种含氟嘧啶类化合物烷氧羰酰化的方法
WO2008131062A2 (en) * 2007-04-20 2008-10-30 Dr. Reddy's Laboratories Ltd. Process for preparing capecitabine
WO2008145403A1 (en) * 2007-06-01 2008-12-04 Synthon B.V. Processes related to making capecitabine
WO2009066892A1 (en) * 2007-11-19 2009-05-28 Hanmi Pharm. Co., Ltd. Methods for preparing capecitabine and beta-anomer-rich trialkyl carbonate compound used therein

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
NOBUO SHIMMA,等: "The Design and Synthesis of a New Tumor-Selective Fluoropyrimidine Carbamate, Capecitabine", 《BIOORGANIC & MEDICINAL CHEMISTRY》 *

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103910773A (zh) * 2014-04-08 2014-07-09 宁波美诺华药业股份有限公司 卡培他滨杂质的合成方法
CN103910773B (zh) * 2014-04-08 2015-11-25 宁波美诺华药业股份有限公司 卡培他滨杂质的合成方法
CN106496294A (zh) * 2016-09-21 2017-03-15 齐鲁天和惠世制药有限公司 一种制备微粉型卡培他滨的方法
CN106496294B (zh) * 2016-09-21 2018-10-30 齐鲁天和惠世制药有限公司 一种制备微粉型卡培他滨的方法
CN107936075A (zh) * 2017-12-28 2018-04-20 山东铂源药业有限公司 一种卡培他滨中间体的合成方法
CN109651466A (zh) * 2018-12-20 2019-04-19 深圳市祥根生物科技有限公司 卡培他滨杂质g的制备方法

Also Published As

Publication number Publication date
KR20120037932A (ko) 2012-04-20
EP2456778A1 (en) 2012-05-30
AR077498A1 (es) 2011-08-31
TW201103550A (en) 2011-02-01
JP2012533618A (ja) 2012-12-27
WO2011010967A1 (en) 2011-01-27
US20110021769A1 (en) 2011-01-27
EP2456778A4 (en) 2013-05-29

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Application publication date: 20130102