CN104114542B - 三唑并嘧啶化合物的合成 - Google Patents

三唑并嘧啶化合物的合成 Download PDF

Info

Publication number
CN104114542B
CN104114542B CN201280069533.4A CN201280069533A CN104114542B CN 104114542 B CN104114542 B CN 104114542B CN 201280069533 A CN201280069533 A CN 201280069533A CN 104114542 B CN104114542 B CN 104114542B
Authority
CN
China
Prior art keywords
compound
formula
salt
tert
iii
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
CN201280069533.4A
Other languages
English (en)
Chinese (zh)
Other versions
CN104114542A (zh
Inventor
N·马拉斯
斯米洛维奇 I·加齐奇
D·施特克
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Lek Pharmaceuticals dd
Original Assignee
Lek Pharmaceuticals dd
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
Priority claimed from EP11195508.4A external-priority patent/EP2607355A1/en
Application filed by Lek Pharmaceuticals dd filed Critical Lek Pharmaceuticals dd
Publication of CN104114542A publication Critical patent/CN104114542A/zh
Application granted granted Critical
Publication of CN104114542B publication Critical patent/CN104114542B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/24—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a ring other than a six-membered aromatic ring
    • 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
    • C07D239/48—Two nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D317/00—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/44—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/06—Systems containing only non-condensed rings with a five-membered ring
    • C07C2601/08—Systems containing only non-condensed rings with a five-membered ring the ring being saturated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/06—Systems containing only non-condensed rings with a five-membered ring
    • C07C2601/10—Systems containing only non-condensed rings with a five-membered ring the ring being unsaturated

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN201280069533.4A 2011-12-23 2012-12-20 三唑并嘧啶化合物的合成 Expired - Fee Related CN104114542B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP11195508.4A EP2607355A1 (en) 2011-12-23 2011-12-23 Synthesis of triazolopyrimidine compounds
EP11195508.4 2011-12-23
EP12169185.1 2012-05-24
EP12169185 2012-05-24
PCT/EP2012/076458 WO2013092900A1 (en) 2011-12-23 2012-12-20 Synthesis of triazolopyrimidine compounds

Publications (2)

Publication Number Publication Date
CN104114542A CN104114542A (zh) 2014-10-22
CN104114542B true CN104114542B (zh) 2017-11-14

Family

ID=47520984

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201280069533.4A Expired - Fee Related CN104114542B (zh) 2011-12-23 2012-12-20 三唑并嘧啶化合物的合成

Country Status (6)

Country Link
US (1) US9278972B2 (enExample)
EP (1) EP2794575B1 (enExample)
CN (1) CN104114542B (enExample)
CA (1) CA2859580A1 (enExample)
IN (1) IN2014KN01491A (enExample)
WO (1) WO2013092900A1 (enExample)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CZ307217B6 (cs) * 2013-03-14 2018-04-04 Zentiva, K.S. Zlepšený způsob výroby a nové intermediáty syntézy ticagreloru
CN104098553B (zh) * 2013-04-10 2017-11-28 江苏恒瑞医药股份有限公司 替格瑞洛的中间体及其制备方法和替格瑞洛的制备方法
CN104610237B (zh) * 2013-11-05 2018-03-30 正大天晴药业集团股份有限公司 一种替格瑞洛的制备方法及其中间体
CN103588750B (zh) * 2013-11-07 2014-11-26 苏州明锐医药科技有限公司 替卡格雷中间体的制备方法
CZ2013866A3 (cs) * 2013-11-08 2015-05-20 Zentiva, K.S. Způsob výroby a nová krystalická forma intermediátu syntézy ticagreloru
CN104710425B (zh) * 2013-12-16 2019-06-14 石药集团中奇制药技术（石家庄）有限公司 一种替格瑞洛新结晶及其制备方法
US10905691B2 (en) 2016-09-09 2021-02-02 Université de Liège Use of triazolo(4,5-d)pyrimidine derivatives for prevention and treatment of bacterial infection
ES2731658T3 (es) * 2016-09-09 2019-11-18 Univ Liege Derivados triazolo(4,5-d)pirimidina para uso en la prevención y tratamiento de infección bacteriana
WO2019169111A1 (en) 2018-03-02 2019-09-06 The Trustees Of The University Of Pennsylvania [1,2,4]triazolo[1,5-a]pyrimidine compounds and use in stabilizing microtubules
CN109896934A (zh) * 2019-03-08 2019-06-18 山东省药学科学院 一种高纯度2-苄氧基溴乙烷的制备方法
CN110467619A (zh) * 2019-08-08 2019-11-19 山西德元堂药业有限公司 一种替格瑞洛的制备方法
CN112047919B (zh) * 2020-09-16 2021-06-18 常州制药厂有限公司 一种替卡格雷中间体及其制备方法
CN113801090B (zh) * 2021-11-18 2022-02-18 南京威凯尔生物医药科技有限公司 一种替格瑞洛关键中间体及其制备方法
CN115537433A (zh) * 2022-11-09 2022-12-30 重庆普佑生物医药有限公司 替卡格雷中间体及其制备方法
CN117105904A (zh) * 2023-08-03 2023-11-24 四川青木制药有限公司 一种替格瑞洛关键中间体的制备方法

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1128801C (zh) * 1998-12-04 2003-11-26 阿斯特拉曾尼卡有限公司 新的三唑并(4,5－d)嘧啶化合物
WO2011017108A2 (en) * 2009-07-27 2011-02-10 Auspex Pharmaceuticals, Inc. Cyclopropyl modulators of p2y12 receptor
CN102149716A (zh) * 2008-09-09 2011-08-10 阿斯利康(瑞典)有限公司 制备[1S-[1α,2α,3β(1S*，2R*),5β]]-3-[7-[2-(3,4-二氟苯基)-环丙氨基]-5-(丙硫基)-3H-1,2,3-三唑并[4,5-d]嘧啶-3-基]-5-(2-羟乙氧基)环戊烷-1,2-二醇的方法及其中间体
CN102731467A (zh) * 2011-04-15 2012-10-17 博瑞生物医药技术(苏州)有限公司 替卡格雷的中间体及制备替卡格雷的方法

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0013488D0 (en) 2000-06-02 2000-07-26 Astrazeneca Ab Chemical compound
WO2011023374A1 (en) 2009-08-31 2011-03-03 Lonza Ltd Process for the preparation of (1s,4r)-2-oxa-3-azabicyclo[2,2.1]hept-5-enes
WO2012138981A2 (en) * 2011-04-06 2012-10-11 Teva Pharmaceutical Industries Ltd. New intermediates and processes for preparing ticagrelor
PL2755957T4 (pl) * 2011-09-14 2017-05-31 Lek Pharmaceuticals D.D. Synteza związków triazolopirymidynowych

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1128801C (zh) * 1998-12-04 2003-11-26 阿斯特拉曾尼卡有限公司 新的三唑并(4,5－d)嘧啶化合物
CN102149716A (zh) * 2008-09-09 2011-08-10 阿斯利康(瑞典)有限公司 制备[1S-[1α,2α,3β(1S*，2R*),5β]]-3-[7-[2-(3,4-二氟苯基)-环丙氨基]-5-(丙硫基)-3H-1,2,3-三唑并[4,5-d]嘧啶-3-基]-5-(2-羟乙氧基)环戊烷-1,2-二醇的方法及其中间体
WO2011017108A2 (en) * 2009-07-27 2011-02-10 Auspex Pharmaceuticals, Inc. Cyclopropyl modulators of p2y12 receptor
CN102731467A (zh) * 2011-04-15 2012-10-17 博瑞生物医药技术(苏州)有限公司 替卡格雷的中间体及制备替卡格雷的方法

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
Carba-nucleosides as Potent Antagonists of the Adenosine 5’-Diphosphate (ADP) Purinergic Receptor (P2Y12) on Human Platelets;Hong Ye et al;《ChemMedChem》;20080125;第3卷;732-736，第733页Scheme 2 *
From ATP to AZD6140: The discovery of an orally active reversible P2Y12 receptor antagonist for the prevention of thrombosis;Brian Springthorpe et al;《Bioorganic & Medicinal Chemistry Letters》;20070819;第17卷;6013-6018 *

Also Published As

Publication number Publication date
IN2014KN01491A (enExample) 2015-10-23
CA2859580A1 (en) 2013-06-27
US9278972B2 (en) 2016-03-08
CN104114542A (zh) 2014-10-22
WO2013092900A1 (en) 2013-06-27
US20140371449A1 (en) 2014-12-18
EP2794575B1 (en) 2018-12-05
EP2794575A1 (en) 2014-10-29

Similar Documents

Publication Publication Date Title
CN104114542B (zh) 三唑并嘧啶化合物的合成
CN104024229B (zh) 三唑并嘧啶化合物的合成
TWI658042B (zh) 雜環化合物的合成
CN101959870B (zh) 吗啉衍生物的制备
CN108699063A (zh) 一种芦可替尼的合成工艺
WO2015010436A1 (zh) 一种Carfilzomib中间体及其制备方法和制备Carfilzomib的方法
WO2014005443A1 (zh) 一种制备选择性抗凝血药替卡格雷及其中间体的方法
KR20120084622A (ko) 시타글립틴의 중간체 제조방법
TWI808068B (zh) 製備3-經取代5-胺基-6H-噻唑并[4,5-d]嘧啶-2,7-二酮化合物之方法
TWI305774B (enExample)
WO2022214645A1 (en) Processes and intermediates for the preparation of relugolix
CN106458892A (zh) 用于制备倍癌霉素前药的改进方法
CN105392772B (zh) 奥格列汀的关键中间体的制备方法
JP2025502931A (ja) 薬物－リンカー複合体の調製方法
CN104520278A (zh) 三唑并嘧啶碳核苷的中间体的制备方法
EP2666771A1 (en) Synthesis of Aminocyclopentanetriol Derivatives
CN107200741A (zh) 一种间变性淋巴瘤激酶抑制剂的制备方法
KR102477924B1 (ko) 인돌 카르복스아미드 화합물을 제조하는 방법
US12006291B2 (en) Processes for the preparation of 4,6,7-trifluoro-1H-indole-2-carboxylic acid
EP2607355A1 (en) Synthesis of triazolopyrimidine compounds
HK1225388A1 (zh) 通过环化2-(氨基乙氧基)苯甲酸衍生物制备3，4-二氢-1，4-苯并氧氮杂环庚三烯-5(2h)-酮衍生物
WO2020134212A1 (zh) 常山酮及其中间体的合成方法
JP2017516790A (ja) Ａｚｄ５３６３の製造方法およびそれに用いられる新規中間体
CN101218218A (zh) 新型焦儿茶酚衍生物
CN119080744A (zh) 一种shp2抑制剂arry-558的制备方法

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
GR01 Patent grant
GR01 Patent grant
CF01 Termination of patent right due to non-payment of annual fee
CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20171114