AR046077A1 - DERIVATIVES OF N4- OXICARBONILCITIMIDINE, ELEABORATION PROCEDURES AND USES OF THE SAME - Google Patents

DERIVATIVES OF N4- OXICARBONILCITIMIDINE, ELEABORATION PROCEDURES AND USES OF THE SAME

Info

Publication number
AR046077A1
AR046077A1 ARP040102558A ARP040102558A AR046077A1 AR 046077 A1 AR046077 A1 AR 046077A1 AR P040102558 A ARP040102558 A AR P040102558A AR P040102558 A ARP040102558 A AR P040102558A AR 046077 A1 AR046077 A1 AR 046077A1
Authority
AR
Argentina
Prior art keywords
derivatives
cycloalkyl
citimidine
oxicarbonilcitimidine
eleaboration
Prior art date
Application number
ARP040102558A
Other languages
Spanish (es)
Inventor
Li Jinliang
He Baofang
Shao Lanying
Wang Lei
Original Assignee
Shangai Desano Chemical Pharma
Shangai Desano Pharmaceutcal H
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
Application filed by Shangai Desano Chemical Pharma, Shangai Desano Pharmaceutcal H filed Critical Shangai Desano Chemical Pharma
Publication of AR046077A1 publication Critical patent/AR046077A1/en

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
    • C07H19/06—Pyrimidine radicals
    • 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
    • C07D239/20—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D239/22—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms directly attached to ring carbon atoms
    • 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)

Abstract

Se revelan derivados de N4-oxicarbonil-citimidina de fórmula general (1) y su preparación. También se revelan esquemas de reacción para preparar el medicamento anticáncer carbamato de fluorocitosina, capecitabina. Estos esquemas de reacción presentan las ventajas de su bajo costo y la gran calidad y alto rendimiento del producto obtenido. Reivindicación 1: Derivados de citimidina, caracterizados porque poseen la estructura de fórmula general (1), donde R1 representa grupos alquilo, cicloalquilo, alquenilo, aralquilo o arilo; R2 representa grupos halógeno, de preferencia flúor o yodo, o un grupo vinilo, etinilo o vinil/etinilo sustituido por halógeno, alquilo, cicloalquilo, cicloalquilo aromático o un radical aromático heterocíclico.N4-Oxycarbonyl-Citimidine derivatives of the general formula (1) and their preparation are disclosed. Reaction schemes are also disclosed to prepare the anti-cancer drug fluorocytosine carbamate, capecitabine. These reaction schemes have the advantages of their low cost and the high quality and high performance of the product obtained. Claim 1: Citimidine derivatives, characterized in that they have the structure of the general formula (1), wherein R 1 represents alkyl, cycloalkyl, alkenyl, aralkyl or aryl groups; R2 represents halogen groups, preferably fluorine or iodine, or a vinyl, ethynyl or vinyl / ethynyl group substituted by halogen, alkyl, cycloalkyl, aromatic cycloalkyl or a heterocyclic aromatic radical.

ARP040102558A 2004-02-23 2004-07-20 DERIVATIVES OF N4- OXICARBONILCITIMIDINE, ELEABORATION PROCEDURES AND USES OF THE SAME AR046077A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CNB2004100164722A CN100383128C (en) 2004-02-23 2004-02-23 Ramification of N-carbethoxy cytosine and preparation method and application

Publications (1)

Publication Number Publication Date
AR046077A1 true AR046077A1 (en) 2005-11-23

Family

ID=34868233

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP040102558A AR046077A1 (en) 2004-02-23 2004-07-20 DERIVATIVES OF N4- OXICARBONILCITIMIDINE, ELEABORATION PROCEDURES AND USES OF THE SAME

Country Status (3)

Country Link
CN (1) CN100383128C (en)
AR (1) AR046077A1 (en)
WO (1) WO2005080351A1 (en)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BRPI0810067A2 (en) 2007-04-20 2014-10-21 Reddys Lab Ltd Dr PROCESS FOR PREPARING CAPECITABIN
AR064165A1 (en) * 2007-12-06 2009-03-18 Richmond Sa Com Ind Y Financie A PROCEDURE FOR THE PREPARATION OF CAPECITABIN AND INTERMEDIARIES USED IN THIS PROCEDURE
CN101469008B (en) * 2007-12-29 2013-08-07 上海特化医药科技有限公司 Capecitabine hydroxy derivatives, preparation thereof and use in capecitabine preparation
WO2009094847A1 (en) * 2007-12-28 2009-08-06 Topharman Shanghai Co., Ltd. A capecitabine hydroxyl-derivative, its preparation processes and uses for preparing capecitabine
WO2009082844A1 (en) * 2007-12-28 2009-07-09 Topharman Shanghai Co., Ltd A capecitabine hydroxyl-derivative, its preparation processes and uses for preparing capecitabine
WO2009082846A1 (en) * 2007-12-28 2009-07-09 Topharman Shanghai Co., Ltd. A capecitabine hydroxyl-derivative, its preparation processes and uses for preparing capecitabine
MX2011001091A (en) 2008-08-01 2011-03-15 Dow Agrosciences Llc Use of 5-fluorocytosine as a fungicide.
WO2010061402A2 (en) * 2008-11-25 2010-06-03 Vishwanath Kannan An improved process for the preparation of capecitabine
EP2210895A1 (en) * 2009-01-27 2010-07-28 F. Hoffmann-La Roche AG Process for the recovery of beta-Acetylfuranoside
CN101987857A (en) * 2009-08-07 2011-03-23 合肥华方医药科技有限公司 Method for synthesizing capecitabine serving as an antineoplastic medicament and intermediate thereof
CN101830953A (en) * 2010-05-26 2010-09-15 南京亚东启天药业有限公司 Method for preparing capecitabine and intermediate thereof
CN101928314A (en) * 2010-08-27 2010-12-29 广东肇庆星湖生物科技股份有限公司 Preparation method for capecitabine
CN102558262A (en) * 2010-12-23 2012-07-11 天津泰普药品科技发展有限公司 Preparation method of high-purity capecitabine
CN102924548B (en) * 2012-11-30 2015-05-20 安润医药科技（苏州）有限公司 Synthesis method of capecitabine
CN103897005B (en) * 2012-12-27 2017-07-28 鲁南制药集团股份有限公司 A kind of method for operating continuously synthesis capecitabine
CN103333119A (en) * 2013-05-28 2013-10-02 中国药科大学 1,2-dihydro-6-methyl-4-substituted amino-5-pyrimidinecarboxylic acid compound and its preparation method and use
CN103772453A (en) * 2014-03-04 2014-05-07 大连大学 Beta-elemene substituted ethyl peracetylated sugar complex, beta-elemene substituted ethyl sugar complex, and preparation methods and use
CN104478975A (en) * 2014-11-24 2015-04-01 苏州乔纳森新材料科技有限公司 Synthesis method of capecitabine
CN104926901B (en) * 2015-06-15 2018-04-20 广安凯特制药有限公司 A kind of synthetic method of capecitabine key intermediate
CN105566419A (en) * 2015-12-28 2016-05-11 上海金和生物技术有限公司 Capecitabine preparation method
CN111072734B (en) * 2019-12-11 2023-04-07 中国科学院昆明植物研究所 Uridine derivative and method for preparing doxifluridine medicament by using same

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA1327358C (en) * 1987-11-17 1994-03-01 Morio Fujiu Fluoro cytidine derivatives
TW254946B (en) * 1992-12-18 1995-08-21 Hoffmann La Roche
US5476932A (en) * 1994-08-26 1995-12-19 Hoffmann-La Roche Inc. Process for producing N4-acyl-5'-deoxy-5-fluorocytidine derivatives
US6005098A (en) * 1998-02-06 1999-12-21 Hoffmann-La Roche Inc. 5'deoxycytidine derivatives

Also Published As

Publication number Publication date
CN100383128C (en) 2008-04-23
WO2005080351A1 (en) 2005-09-01
CN1660819A (en) 2005-08-31

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