CN103619864A - 5-氮杂胞苷的合成 - Google Patents

5-氮杂胞苷的合成 Download PDF

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Publication number
CN103619864A
CN103619864A CN201280026401.3A CN201280026401A CN103619864A CN 103619864 A CN103619864 A CN 103619864A CN 201280026401 A CN201280026401 A CN 201280026401A CN 103619864 A CN103619864 A CN 103619864A
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China
Prior art keywords
azacytidine
salt
less
acid
reaction
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Pending
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CN201280026401.3A
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English (en)
Chinese (zh)
Inventor
奇恩纳皮莱·拉詹迪兰
佩里延迪·纳卡拉占
贾斯提·文卡特斯瓦劳
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Celgene International SARL
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Celgene International SARL
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • 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
    • C07H19/12—Triazine radicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • 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
    • C07H1/00—Processes for the preparation of sugar derivatives
    • C07H1/06—Separation; Purification
    • 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
    • Y02P20/582—Recycling of unreacted starting or intermediate materials

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hematology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oncology (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201280026401.3A 2011-03-31 2012-03-29 5-氮杂胞苷的合成 Pending CN103619864A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161470392P 2011-03-31 2011-03-31
US61/470,392 2011-03-31
PCT/US2012/031059 WO2012135405A1 (en) 2011-03-31 2012-03-29 Systhesis of 5-azacytidine

Publications (1)

Publication Number Publication Date
CN103619864A true CN103619864A (zh) 2014-03-05

Family

ID=46000343

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201280026401.3A Pending CN103619864A (zh) 2011-03-31 2012-03-29 5-氮杂胞苷的合成

Country Status (13)

Country Link
US (1) US9951098B2 (https=)
EP (1) EP2691408B1 (https=)
JP (1) JP6289361B2 (https=)
KR (1) KR20140019820A (https=)
CN (1) CN103619864A (https=)
AU (1) AU2012236476A1 (https=)
BR (1) BR112013025167A2 (https=)
IL (1) IL228604A0 (https=)
MX (1) MX2013010945A (https=)
RU (1) RU2013148580A (https=)
SG (1) SG193622A1 (https=)
WO (1) WO2012135405A1 (https=)
ZA (1) ZA201307142B (https=)

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN108368148A (zh) * 2016-04-21 2018-08-03 大原药品工业株式会社 5-氮杂胞苷的糖部分甲硅烷基醚衍生物
CN109305992A (zh) * 2017-07-28 2019-02-05 江苏先声药业有限公司 一种阿扎胞苷的制备方法
CN109988207A (zh) * 2017-12-29 2019-07-09 江苏豪森药业集团有限公司 阿扎胞苷晶型的制备方法
CN110092807A (zh) * 2018-01-30 2019-08-06 中国医学科学院药物研究所 一种高纯、低灼烧残渣的制备阿扎胞苷的方法
CN113201039A (zh) * 2021-05-19 2021-08-03 南京德克瑞医药化工有限公司 一种医药中间体2’,3’,5’-三乙酰阿扎胞苷的制备方法

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EP3782612B1 (en) 2008-05-15 2023-11-08 Celgene Corporation Oral formulations of cytidine analogs and methods of use thereof
WO2012106299A1 (en) 2011-01-31 2012-08-09 Celgene Corporation Pharmaceutical compositions of cytidine analogs and methods of use thereof
US9968627B2 (en) 2013-03-26 2018-05-15 Celgene Corporation Solid forms comprising 4-amino-1-β-D-ribofuranosyl-1,3,5-triazin-2(1H)-one and a coformer, compositions and methods of use thereof
WO2014169216A2 (en) 2013-04-11 2014-10-16 Carnegie Mellon University TEMPLATE-DIRECTED γPNA SYNTHESIS AND γPNA TARGETING COMPOUNDS
WO2014169206A2 (en) 2013-04-11 2014-10-16 Carnegie Mellon University Divalent nucleobase compounds and uses therefor
CN103450303A (zh) * 2013-09-04 2013-12-18 重庆泰濠制药有限公司 阿扎胞苷晶型a、阿扎胞苷晶型b及其制备方法
CN104672289A (zh) * 2013-11-29 2015-06-03 南京圣和药业股份有限公司 一种阿扎胞苷杂质的制备方法
CN114907272A (zh) 2016-09-26 2022-08-16 卡耐基梅隆大学 二价核碱基化合物及其用途
JP7017638B2 (ja) 2018-02-07 2022-02-08 ラブレス バイオメディカル リサーチ インスティテュート 吸入可能な乾燥粉末シチジン類似体組成物及び癌への治療として使用する方法
KR20190136284A (ko) * 2018-05-30 2019-12-10 주식회사 삼양바이오팜 안정한 아자시티딘-함유 약제학적 조성물의 제조방법
WO2022113069A1 (en) 2020-11-24 2022-06-02 Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd. E protein channel blockers and orf3 inhibitors as anti-covid-19 agents
BR112022022243A2 (pt) 2020-05-01 2022-12-20 Yissum Res Dev Co Of Hebrew Univ Jerusalem Ltd Bloqueadores do canal de proteína e e inibidores de orf3 como agentes anti-covid-19.
AR134497A1 (es) 2023-11-28 2026-01-21 Sanofi Sa Combiterapia multifuncional con activador de los linfocitos citolíticos naturales (nk) para tratar trastornos neoplásicos hemáticos

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WO2006034154A2 (en) * 2004-09-17 2006-03-30 Supergen, Inc. Salts of 5-azacytidine
WO2008088779A2 (en) * 2007-01-11 2008-07-24 Ivax Pharmaceuticals S.R.O. Solid state forms of 5-azacytidine and processes for preparation thereof

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FR2123632A6 (en) 1971-01-26 1972-09-15 Ceskoslovenska Akademie Ved Prepn of 5-azacytosines and 5-azacytidines - from bis trimethylsilyl-5-azacytosine
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Cited By (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN108368148A (zh) * 2016-04-21 2018-08-03 大原药品工业株式会社 5-氮杂胞苷的糖部分甲硅烷基醚衍生物
CN108368148B (zh) * 2016-04-21 2021-11-05 大原药品工业株式会社 5-氮杂胞苷的糖部分甲硅烷基醚衍生物
CN109305992A (zh) * 2017-07-28 2019-02-05 江苏先声药业有限公司 一种阿扎胞苷的制备方法
CN109988207A (zh) * 2017-12-29 2019-07-09 江苏豪森药业集团有限公司 阿扎胞苷晶型的制备方法
CN109988207B (zh) * 2017-12-29 2022-01-04 江苏豪森药业集团有限公司 阿扎胞苷晶型的制备方法
CN110092807A (zh) * 2018-01-30 2019-08-06 中国医学科学院药物研究所 一种高纯、低灼烧残渣的制备阿扎胞苷的方法
CN113201039A (zh) * 2021-05-19 2021-08-03 南京德克瑞医药化工有限公司 一种医药中间体2’,3’,5’-三乙酰阿扎胞苷的制备方法
CN113201039B (zh) * 2021-05-19 2022-04-29 南京德克瑞医药化工有限公司 一种医药中间体2’,3’,5’-三乙酰阿扎胞苷的制备方法

Also Published As

Publication number Publication date
JP6289361B2 (ja) 2018-03-07
SG193622A1 (en) 2013-11-29
IL228604A0 (en) 2013-12-31
WO2012135405A1 (en) 2012-10-04
ZA201307142B (en) 2015-11-25
EP2691408B1 (en) 2017-06-28
EP2691408A1 (en) 2014-02-05
KR20140019820A (ko) 2014-02-17
BR112013025167A2 (pt) 2019-09-24
JP2014510755A (ja) 2014-05-01
RU2013148580A (ru) 2015-05-10
US20140128593A1 (en) 2014-05-08
US9951098B2 (en) 2018-04-24
MX2013010945A (es) 2014-03-12
AU2012236476A1 (en) 2013-05-02

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Application publication date: 20140305