EA201070437A2 - Способ получения 2'-дезокси -5-азацитидина (децитабина) - Google Patents

Способ получения 2'-дезокси -5-азацитидина (децитабина)

Info

Publication number
EA201070437A2
EA201070437A2 EA201070437A EA201070437A EA201070437A2 EA 201070437 A2 EA201070437 A2 EA 201070437A2 EA 201070437 A EA201070437 A EA 201070437A EA 201070437 A EA201070437 A EA 201070437A EA 201070437 A2 EA201070437 A2 EA 201070437A2
Authority
EA
Eurasian Patent Office
Prior art keywords
compound
formula
decitabine
deoxy
azacitidine
Prior art date
Application number
EA201070437A
Other languages
English (en)
Other versions
EA018924B1 (ru
EA201070437A3 (ru
Inventor
Оливер Юнгманн
Норберт Краут
Original Assignee
Цилаг Аг
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.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=39496166&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=EA201070437(A2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Цилаг Аг filed Critical Цилаг Аг
Publication of EA201070437A2 publication Critical patent/EA201070437A2/ru
Publication of EA201070437A3 publication Critical patent/EA201070437A3/ru
Publication of EA018924B1 publication Critical patent/EA018924B1/ru

Links

Classifications

    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Molecular Biology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biochemistry (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Saccharide Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Catalysts (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Способ получения 2'-дезокси-5-азацитидина (децитабина) путем предоставления соединения формулы (I), в которой R представляет собой удаляемый заместитель, известный per se; a Rпредставляет собой удаляемый заместитель; далее, предоставления силилированного основания формулы (II), в которой Rпредставляет собой защитную группу, предпочтительно триметилсилильный (TMS) остаток; осуществления взаимодействия соединения формулы (I) и соединения формулы (II) в подходящем безводном растворителе и в присутствии подходящего катализатора; и удаления заместителей R из полученного соединения с получением указанного соединения, представляющего собой 2'-дезокси-5-азацитидин (децитабин), при этом указанный катализатор выбирают из группы, включающей соль алифатической сульфокислоты или соль сильной неорганической кислоты.
EA201070437A 2007-10-10 2008-10-10 Способ получения 2'-дезокси-5-азацитидина (децитабина) EA018924B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP07019826A EP2050757A1 (en) 2007-10-10 2007-10-10 Method of producing 2' -deoxy-5-azacytidine (Decitabine)
PCT/EP2008/063581 WO2009047313A2 (en) 2007-10-10 2008-10-10 Method of producing 2' -deoxy-5-azacytidine (decitabine)

Publications (3)

Publication Number Publication Date
EA201070437A2 true EA201070437A2 (ru) 2010-08-30
EA201070437A3 EA201070437A3 (ru) 2011-02-28
EA018924B1 EA018924B1 (ru) 2013-11-29

Family

ID=39496166

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201070437A EA018924B1 (ru) 2007-10-10 2008-10-10 Способ получения 2'-дезокси-5-азацитидина (децитабина)

Country Status (32)

Country Link
US (1) US20100222565A1 (ru)
EP (2) EP2050757A1 (ru)
JP (1) JP5453279B2 (ru)
KR (1) KR101551779B1 (ru)
CN (1) CN102037003B (ru)
AP (1) AP2719A (ru)
AU (1) AU2008309552B2 (ru)
BR (1) BRPI0818595B1 (ru)
CA (1) CA2703560C (ru)
CO (1) CO6270260A2 (ru)
CY (1) CY1116540T1 (ru)
DK (1) DK2201020T3 (ru)
EA (1) EA018924B1 (ru)
EC (1) ECSP10010091A (ru)
ES (1) ES2512591T3 (ru)
GT (1) GT201000076A (ru)
HK (1) HK1152312A1 (ru)
HN (1) HN2010000654A (ru)
HR (1) HRP20140856T1 (ru)
IL (1) IL204918A0 (ru)
MX (1) MX2010003887A (ru)
MY (1) MY150047A (ru)
NI (1) NI201000049A (ru)
NZ (1) NZ584373A (ru)
PL (1) PL2201020T3 (ru)
PT (1) PT2201020E (ru)
SI (1) SI2201020T1 (ru)
SV (1) SV2010003523A (ru)
UA (1) UA101482C2 (ru)
UY (1) UY31388A1 (ru)
WO (1) WO2009047313A2 (ru)
ZA (1) ZA201002517B (ru)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2048151A1 (en) * 2007-10-10 2009-04-15 Cilag AG Method for producing nucleosides by direct glycosylation of the nucleoside base
US8586729B2 (en) 2008-10-03 2013-11-19 Scinopharm Taiwan Ltd. Synthesis of decitabine
AR076418A1 (es) * 2009-04-27 2011-06-08 Reddys Lab Inc Dr Preparacion de decitabina
IT1399195B1 (it) * 2010-03-30 2013-04-11 Chemi Spa Processo per la sintesi di azacitidina e decitabina
CN101948493A (zh) * 2010-06-28 2011-01-19 江苏奥赛康药业有限公司 一种高纯度地西他滨的工业化生产方法
KR101241321B1 (ko) * 2010-08-05 2013-03-11 케이피엑스 라이프사이언스 주식회사 수율 및 순도가 개선된 데시타빈의 제조방법
CN102391338A (zh) * 2011-09-30 2012-03-28 重庆泰濠制药有限公司 一种地西他滨中间体粗品的纯化方法
CN104211743A (zh) * 2013-05-29 2014-12-17 南京工业大学 一种地西他宾的合成
CN103601768B (zh) * 2013-11-13 2015-09-30 齐鲁天和惠世制药有限公司 一种阿米卡星的制备方法
EP3383406B1 (en) * 2015-12-03 2021-10-20 Epidestiny, Inc. Compositions containing decitabine, 5-azacytidine and tetrahydrouridine and uses thereof
CN109912672B (zh) * 2019-04-02 2021-07-27 江西师范大学 一种以邻炔基苯酚醚作为离去基的碱基糖苷化的方法
CN112209976B (zh) * 2019-07-10 2023-05-26 鲁南制药集团股份有限公司 一种地西他滨中间体化合物ⅴ
CN112209977B (zh) * 2019-07-10 2023-05-26 鲁南制药集团股份有限公司 一种地西他滨中间体化合物ⅵ

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2012888C3 (de) * 1970-03-14 1981-04-02 Schering Ag, 1000 Berlin Und 4619 Bergkamen Verfahren zur Herstellung von 5-Azapyrimidinnucleosiden
DE2508312A1 (de) * 1975-02-24 1976-09-02 Schering Ag Neues verfahren zur herstellung von nucleosiden
DE2757365A1 (de) * 1977-12-20 1979-06-21 Schering Ag Neues verfahren zur herstellung von nucleosiden
US5426183A (en) * 1992-06-22 1995-06-20 Eli Lilly And Company Catalytic stereoselective glycosylation process for preparing 2'-deoxy-2',2'-difluoronucleosides and 2'-deoxy-2'-fluoronucleosides
UA41261C2 (uk) * 1992-06-22 2001-09-17 Елі Ліллі Енд Компані Спосіб одержання збагачених бета-аномером нуклеозидів
US5606048A (en) 1992-06-22 1997-02-25 Eli Lilly And Company Stereoselective glycosylation process for preparing 2'-Deoxy-2', 2'-difluoronucleosides and 2'-deoxy-2'-fluoronucleosides
US5811540A (en) * 1993-11-05 1998-09-22 The Noguchi Institute 5-O-pyrimidyl-2,3-dideoxy-1-thiofuranoside derivative, and production method and use thereof
KR100213932B1 (ko) * 1995-11-02 1999-08-02 김충환 새로운 뉴클레오시드 유도체 및 그 제조방법
EP1104415B1 (en) * 1998-08-12 2004-11-10 Gilead Sciences, Inc. Method of manufacture of 1,3-oxathiolane nucleosides

Also Published As

Publication number Publication date
EP2050757A1 (en) 2009-04-22
CY1116540T1 (el) 2017-03-15
HN2010000654A (es) 2012-12-03
KR20100064387A (ko) 2010-06-14
EA018924B1 (ru) 2013-11-29
NZ584373A (en) 2011-08-26
AU2008309552A1 (en) 2009-04-16
UA101482C2 (ru) 2013-04-10
KR101551779B1 (ko) 2015-09-09
JP5453279B2 (ja) 2014-03-26
CA2703560A1 (en) 2009-04-16
AP2010005226A0 (en) 2010-04-30
AP2719A (en) 2013-07-31
BRPI0818595A2 (pt) 2015-04-22
MX2010003887A (es) 2010-04-30
NI201000049A (es) 2010-11-10
BRPI0818595B1 (pt) 2022-02-15
WO2009047313A2 (en) 2009-04-16
DK2201020T3 (da) 2014-10-13
IL204918A0 (en) 2010-11-30
ES2512591T3 (es) 2014-10-24
ECSP10010091A (es) 2010-06-29
SV2010003523A (es) 2011-01-25
PL2201020T3 (pl) 2014-12-31
CN102037003B (zh) 2014-05-07
HK1152312A1 (en) 2012-02-24
CN102037003A (zh) 2011-04-27
PT2201020E (pt) 2014-09-23
EP2201020B1 (en) 2014-07-16
EA201070437A3 (ru) 2011-02-28
GT201000076A (es) 2012-03-12
CO6270260A2 (es) 2011-04-20
CA2703560C (en) 2016-09-13
US20100222565A1 (en) 2010-09-02
UY31388A1 (es) 2009-04-30
JP2011518759A (ja) 2011-06-30
SI2201020T1 (sl) 2014-11-28
WO2009047313A3 (en) 2012-03-01
AU2008309552B2 (en) 2013-01-17
EP2201020A2 (en) 2010-06-30
ZA201002517B (en) 2012-07-25
HRP20140856T1 (hr) 2014-10-24
MY150047A (en) 2013-11-29

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