CN104093702A - 用于制备药物试剂的方法和中间体 - Google Patents

用于制备药物试剂的方法和中间体 Download PDF

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Publication number
CN104093702A
CN104093702A CN201380007712.XA CN201380007712A CN104093702A CN 104093702 A CN104093702 A CN 104093702A CN 201380007712 A CN201380007712 A CN 201380007712A CN 104093702 A CN104093702 A CN 104093702A
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formula
compound
salt
alkyl
compounds
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English (en)
Chinese (zh)
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A·J·库伦
余洪超
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Gilead Sciences Inc
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Gilead Sciences Inc
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • 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
    • C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/12—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
    • 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
    • C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/16—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by singly-bound oxygen atoms
    • 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
    • C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/20—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by nitrogen atoms not being part of nitro or nitroso groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/63—Esters of sulfonic acids
    • C07C309/72—Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/73—Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton to carbon atoms of non-condensed six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C329/00—Thiocarbonic acids; Halides, esters or anhydrides thereof
    • C07C329/12—Dithiocarbonic acids; Derivatives thereof
    • C07C329/14—Esters of dithiocarbonic acids
    • C07C329/16—Esters of dithiocarbonic acids having sulfur atoms of dithiocarbonic groups bound to acyclic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D203/00—Heterocyclic compounds containing three-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D203/04—Heterocyclic compounds containing three-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D203/06—Heterocyclic compounds containing three-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D203/16—Heterocyclic compounds containing three-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with acylated ring nitrogen atoms
    • C07D203/20—Heterocyclic compounds containing three-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with acylated ring nitrogen atoms by carbonic acid, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • C07D233/60—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with hydrocarbon radicals, substituted by oxygen or sulfur atoms, attached to ring nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D277/24—Radicals substituted by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D277/28—Radicals substituted by nitrogen atoms

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Health & Medical Sciences (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Virology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Communicable Diseases (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201380007712.XA 2012-02-03 2013-02-01 用于制备药物试剂的方法和中间体 Pending CN104093702A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261594686P 2012-02-03 2012-02-03
US61/594,686 2012-02-03
PCT/US2013/024431 WO2013116715A1 (en) 2012-02-03 2013-02-01 Methods and intermediates for preparing pharmaceutical agents

Publications (1)

Publication Number Publication Date
CN104093702A true CN104093702A (zh) 2014-10-08

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CN201380007712.XA Pending CN104093702A (zh) 2012-02-03 2013-02-01 用于制备药物试剂的方法和中间体

Country Status (15)

Country Link
US (1) US9346796B2 (2)
EP (1) EP2809646A1 (2)
JP (1) JP2015510509A (2)
KR (1) KR20140128392A (2)
CN (1) CN104093702A (2)
AU (1) AU2013214879A1 (2)
BR (1) BR112014018738A8 (2)
CA (1) CA2862344A1 (2)
HK (1) HK1205095A1 (2)
IL (1) IL233654A0 (2)
IN (1) IN2014DN06192A (2)
MX (1) MX2014009344A (2)
RU (1) RU2014129937A (2)
SG (2) SG10201509336RA (2)
WO (1) WO2013116715A1 (2)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104557565A (zh) * 2015-01-08 2015-04-29 浙江工业大学 抗艾滋病药物增强剂Cobicistat关键中间体盐酸盐的制备方法
CN107513046A (zh) * 2016-06-15 2017-12-26 江苏福瑞生物医药有限公司 一种可比司他的合成方法
CN112500367A (zh) * 2020-12-16 2021-03-16 盐城迪赛诺制药有限公司 一种利托那韦中间体的精制方法
CN112592324A (zh) * 2020-12-16 2021-04-02 盐城迪赛诺制药有限公司 一种纯化利托那韦中间体原料的方法

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104370777A (zh) * 2013-08-13 2015-02-25 上海迪赛诺化学制药有限公司 合成(2r,5r)-1,6-二苯基己烷-2,5-二胺及其盐的中间体及所述中间体的制备方法和应用
US9975864B2 (en) 2013-12-03 2018-05-22 Mylan Laboratories Limited Preparation of cobicistat intermediates
CN104193643B (zh) * 2014-09-12 2016-02-10 宁波九胜创新医药科技有限公司 用于合成抗艾滋病药物增强剂cobicistat的中间体

Citations (4)

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WO1994014436A1 (en) * 1992-12-29 1994-07-07 Abbott Laboratories Retroviral protease inhibiting compounds
WO2008010921A2 (en) * 2006-07-07 2008-01-24 Gilead Sciences, Inc. Modulators of pharmacokinetic properties of therapeutics
WO2010115000A2 (en) * 2009-04-03 2010-10-07 Gilead Sciences, Inc. Methods and intermediates for preparing pharmaceutical agents
CN101967130A (zh) * 2010-07-02 2011-02-09 厦门市亨瑞生化有限公司 利托那韦中间体的合成方法

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US5142056A (en) 1989-05-23 1992-08-25 Abbott Laboratories Retroviral protease inhibiting compounds
IE20010533A1 (en) 1990-11-20 2003-03-05 Abbott Lab Intermediates for preparing retroviral protease inhibiting compounds
US5763464A (en) * 1995-11-22 1998-06-09 The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services Retroviral agents containing anthranilamide, substituted benzamide and other subunits, and methods of using same
US20030153771A1 (en) 2001-09-27 2003-08-14 Kolb Hartmuth C. Large scale synthesis of optically pure aziridines
WO2003106445A1 (en) 2002-06-12 2003-12-24 Qsi Pharma A/S Compounds and methods for controlling bacterial virulence
EP2465855A1 (en) * 2006-08-31 2012-06-20 Abbott Laboratories Cytochrome P450 oxidase inhibitors and uses thereof
EP4403221A3 (en) 2007-02-23 2024-10-09 Gilead Sciences, Inc. Modulators of pharmacokinetic properties of therapeutics
CN103479584A (zh) 2008-05-02 2014-01-01 吉里德科学公司 固体载体颗粒在改善药物制剂加工性中的应用
US20130280212A1 (en) * 2010-12-21 2013-10-24 Gilead Sciences, Inc Inhibitors of cytochrome p450

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1994014436A1 (en) * 1992-12-29 1994-07-07 Abbott Laboratories Retroviral protease inhibiting compounds
WO2008010921A2 (en) * 2006-07-07 2008-01-24 Gilead Sciences, Inc. Modulators of pharmacokinetic properties of therapeutics
CN101490023A (zh) * 2006-07-07 2009-07-22 吉里德科学公司 治疗剂的药代动力学特性调节剂
WO2010115000A2 (en) * 2009-04-03 2010-10-07 Gilead Sciences, Inc. Methods and intermediates for preparing pharmaceutical agents
CN101967130A (zh) * 2010-07-02 2011-02-09 厦门市亨瑞生化有限公司 利托那韦中间体的合成方法

Non-Patent Citations (3)

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Title
ARUN K. GHOSH等: ""Potent HIV-1Protease Inhibitors: Stereoselective Synthesis of a Dipeptide Mimic"", 《J. ORG. CHEM.》 *
ERRABELLI RAMU等: ""A short approach to the synthesis of the ritonavir and lopinavir core and its C-3 epimer via cross metathesis"", 《TETRAHEDRON: ASYMMETRY》 *
MUKUND K. GURJAR等: ""Synthesis of Novel C2-symmetric and Pseudo C2-symmetric Based Diols, Epoxides and Dideoxy Derivatives of HIV Protease Inhibitors"", 《TETRAHEDRON》 *

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104557565A (zh) * 2015-01-08 2015-04-29 浙江工业大学 抗艾滋病药物增强剂Cobicistat关键中间体盐酸盐的制备方法
CN107513046A (zh) * 2016-06-15 2017-12-26 江苏福瑞生物医药有限公司 一种可比司他的合成方法
CN107513046B (zh) * 2016-06-15 2019-12-13 江苏欧信制药有限公司 一种可比司他的合成方法
CN112500367A (zh) * 2020-12-16 2021-03-16 盐城迪赛诺制药有限公司 一种利托那韦中间体的精制方法
CN112592324A (zh) * 2020-12-16 2021-04-02 盐城迪赛诺制药有限公司 一种纯化利托那韦中间体原料的方法

Also Published As

Publication number Publication date
KR20140128392A (ko) 2014-11-05
BR112014018738A8 (pt) 2017-07-11
RU2014129937A (ru) 2016-03-27
HK1205095A1 (en) 2015-12-11
WO2013116715A1 (en) 2013-08-08
SG10201509336RA (en) 2015-12-30
US20140364602A1 (en) 2014-12-11
BR112014018738A2 (2) 2017-06-20
MX2014009344A (es) 2015-05-11
SG11201404527QA (en) 2014-08-28
CA2862344A1 (en) 2013-08-08
AU2013214879A1 (en) 2014-08-07
IN2014DN06192A (2) 2015-10-23
EP2809646A1 (en) 2014-12-10
IL233654A0 (en) 2014-08-31
JP2015510509A (ja) 2015-04-09
US9346796B2 (en) 2016-05-24

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Application publication date: 20141008