CN104520275B - 用于制备整合酶抑制剂的方法和中间产物 - Google Patents

用于制备整合酶抑制剂的方法和中间产物 Download PDF

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Publication number
CN104520275B
CN104520275B CN201380041287.6A CN201380041287A CN104520275B CN 104520275 B CN104520275 B CN 104520275B CN 201380041287 A CN201380041287 A CN 201380041287A CN 104520275 B CN104520275 B CN 104520275B
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compound
formula
salt
compounds
mixture
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Expired - Fee Related
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CN201380041287.6A
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English (en)
Chinese (zh)
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CN104520275A (zh
Inventor
多米尼卡·皮乔恩
卡丽·托马斯
马克·查理斯·惠特科姆
埃里克·D.·道迪
傅文艺
帕特丽夏·麦克劳德
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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
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D215/54—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3
    • C07D215/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3 with oxygen atoms in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C43/00—Ethers; Compounds having groups, groups or groups
    • C07C43/02—Ethers
    • C07C43/20—Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring
    • C07C43/225—Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring containing halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C43/00—Ethers; Compounds having groups, groups or groups
    • C07C43/02—Ethers
    • C07C43/257—Ethers having an ether-oxygen atom bound to carbon atoms both belonging to six-membered aromatic rings
    • C07C43/29—Ethers having an ether-oxygen atom bound to carbon atoms both belonging to six-membered aromatic rings containing halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/27—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by oxidation
    • C07C45/30—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by oxidation with halogen containing compounds, e.g. hypohalogenation
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/45—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by condensation
    • C07C45/46—Friedel-Crafts reactions
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C49/00—Ketones; Ketenes; Dimeric ketenes; Ketonic chelates
    • C07C49/76—Ketones containing a keto group bound to a six-membered aromatic ring
    • C07C49/84—Ketones containing a keto group bound to a six-membered aromatic ring containing ether groups, groups, groups, or groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C67/00—Preparation of carboxylic acid esters
    • C07C67/12—Preparation of carboxylic acid esters from asymmetrical anhydrides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C67/00—Preparation of carboxylic acid esters
    • C07C67/30—Preparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group
    • C07C67/333—Preparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group by isomerisation; by change of size of the carbon skeleton
    • C07C67/343—Preparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group by isomerisation; by change of size of the carbon skeleton by increase in the number of carbon atoms

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Quinoline Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
CN201380041287.6A 2012-08-03 2013-08-01 用于制备整合酶抑制剂的方法和中间产物 Expired - Fee Related CN104520275B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261679475P 2012-08-03 2012-08-03
US61/679,475 2012-08-03
PCT/US2013/053295 WO2014022707A1 (en) 2012-08-03 2013-08-01 Process and intermediates for preparing integrase inhibitors

Publications (2)

Publication Number Publication Date
CN104520275A CN104520275A (zh) 2015-04-15
CN104520275B true CN104520275B (zh) 2016-11-02

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CN201380041287.6A Expired - Fee Related CN104520275B (zh) 2012-08-03 2013-08-01 用于制备整合酶抑制剂的方法和中间产物

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Country Link
US (1) US8877931B2 (enExample)
EP (1) EP2880017B1 (enExample)
JP (1) JP6147856B2 (enExample)
KR (1) KR20150040340A (enExample)
CN (1) CN104520275B (enExample)
AU (1) AU2013296289B2 (enExample)
BR (1) BR112015002275A2 (enExample)
CA (1) CA2878699C (enExample)
EA (1) EA026089B1 (enExample)
ES (1) ES2608860T3 (enExample)
IL (1) IL236618A (enExample)
IN (1) IN2015DN01688A (enExample)
MX (1) MX337094B (enExample)
NZ (1) NZ630199A (enExample)
PT (1) PT2880017T (enExample)
SG (1) SG11201500812QA (enExample)
WO (1) WO2014022707A1 (enExample)

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SI3067358T1 (sl) 2012-12-21 2019-12-31 Gilead Sciences, Inc. Policiklične spojine karbamoilpiridona in njihova farmacevtska uporaba
AU2014286993B2 (en) 2013-07-12 2018-10-25 Gilead Sciences, Inc. Polycyclic-carbamoylpyridone compounds and their use for the treatment of HIV infections
NO2865735T3 (enExample) 2013-07-12 2018-07-21
TWI744723B (zh) 2014-06-20 2021-11-01 美商基利科學股份有限公司 多環型胺甲醯基吡啶酮化合物之合成
TW201613936A (en) 2014-06-20 2016-04-16 Gilead Sciences Inc Crystalline forms of(2R,5S,13aR)-8-hydroxy-7,9-dioxo-n-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide
NO2717902T3 (enExample) 2014-06-20 2018-06-23
TWI695003B (zh) 2014-12-23 2020-06-01 美商基利科學股份有限公司 多環胺甲醯基吡啶酮化合物及其醫藥用途
CA2980362C (en) 2015-04-02 2020-02-25 Gilead Sciences, Inc. Polycyclic-carbamoylpyridone compounds and their pharmaceutical use
US20220332732A1 (en) * 2019-09-24 2022-10-20 Asymchem Laboratories (Tianjin) Co., Ltd. Continuous preparation method for benzylzinc halide and derivative thereof
CN112661698A (zh) * 2021-01-14 2021-04-16 浙江海森药业股份有限公司 一种艾维雷韦的制备方法

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CN101516819A (zh) * 2006-09-12 2009-08-26 吉里德科学公司 制备整合酶抑制剂的方法和中间体
CN101821223A (zh) * 2007-09-11 2010-09-01 吉里德科学公司 用于制备整合酶抑制剂的方法和中间体

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MXPA03005338A (es) 2000-12-14 2003-10-06 Procter & Gamble Etapa de ciclizacion en el procedimiento de elaboracion de quinolonas y naftiridinas.
TW200300349A (en) 2001-11-19 2003-06-01 Sankyo Co A 4-oxoqinoline derivative
EP1510510A1 (en) 2002-05-31 2005-03-02 Banyu Pharmaceutical Co., Ltd. Method of substituent introduction through halogen-metal exchange reaction
US6803469B2 (en) 2002-08-05 2004-10-12 The Procter & Gamble Company Process for preparing quinolone antibiotic intermediates
TW200409759A (en) 2002-09-25 2004-06-16 Wyeth Corp Substituted 4-(indazol-3-yl)phenols
EP1582523A1 (en) 2004-04-02 2005-10-05 Ludwig-Maximilians-Universität München Method of preparing organomagnesium compounds
EP1582524B1 (en) 2004-04-02 2008-08-13 Ludwig Maximilians Universität Method of preparing organomagnesium compounds
WO2005113509A1 (en) 2004-05-20 2005-12-01 Japan Tobacco Inc. Novel 4-oxoquinoline compound and use thereof as hiv integrase inhibitor
MY134672A (en) 2004-05-20 2007-12-31 Japan Tobacco Inc Stable crystal of 4-oxoquinoline compound
EP3287130A1 (en) 2004-05-21 2018-02-28 Japan Tobacco Inc. Combinations comprising a 4-isoquinolone derivative and protease inhibitors
WO2007063869A1 (ja) 2005-11-30 2007-06-07 Japan Tobacco Inc. 高純度キノロン化合物の製造方法
US20090233964A1 (en) 2005-12-30 2009-09-17 Gilead Sciences, Inc. Methods for improving the pharmacokinetics of hiv integrase inhibitors
WO2007102499A1 (ja) 2006-03-06 2007-09-13 Japan Tobacco Inc. ４－オキソキノリン化合物の製造方法
ES2531190T3 (es) 2006-03-06 2015-03-11 Japan Tobacco Inc Método para producir un compuesto de 4-oxoquinolina
TW200811153A (en) 2006-06-23 2008-03-01 Japan Tobacco Inc 6-(heterocyclyl-substituted benzyl)-4-oxoquinoline compound and use thereof as HIV integrase inhibitor
CN101686972B (zh) 2007-06-29 2013-08-14 吉里德科学公司 治疗用组合物和方法
CN103356622A (zh) 2007-06-29 2013-10-23 吉里德科学公司 治疗用组合物及其用途

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US20050239819A1 (en) * 2002-11-20 2005-10-27 Motohide Satoh 4-Oxoquinoline compounds and utilization thereof as hiv integrase inhibitors
CN101516819A (zh) * 2006-09-12 2009-08-26 吉里德科学公司 制备整合酶抑制剂的方法和中间体
CN101821223A (zh) * 2007-09-11 2010-09-01 吉里德科学公司 用于制备整合酶抑制剂的方法和中间体

Also Published As

Publication number Publication date
WO2014022707A1 (en) 2014-02-06
CN104520275A (zh) 2015-04-15
US8877931B2 (en) 2014-11-04
ES2608860T3 (es) 2017-04-17
PT2880017T (pt) 2016-12-14
EP2880017A1 (en) 2015-06-10
HK1209748A1 (en) 2016-04-08
AU2013296289B2 (en) 2017-10-05
US20140039194A1 (en) 2014-02-06
HK1209415A1 (en) 2016-04-01
EA026089B1 (ru) 2017-02-28
BR112015002275A2 (pt) 2017-07-04
MX2015001506A (es) 2015-04-08
MX337094B (es) 2016-02-10
EA201590018A1 (ru) 2015-05-29
CA2878699C (en) 2018-09-11
SG11201500812QA (en) 2015-04-29
CA2878699A1 (en) 2014-02-06
NZ630199A (en) 2016-12-23
IN2015DN01688A (enExample) 2015-07-03
JP6147856B2 (ja) 2017-06-14
AU2013296289A1 (en) 2015-02-19
IL236618A0 (en) 2015-02-26
EP2880017B1 (en) 2016-10-05
JP2015524822A (ja) 2015-08-27
IL236618A (en) 2017-04-30
KR20150040340A (ko) 2015-04-14

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