ES2608860T3 - Proceso e intermedios para preparar inhibidores de la integrasa - Google Patents

Proceso e intermedios para preparar inhibidores de la integrasa Download PDF

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Publication number
ES2608860T3
ES2608860T3 ES13748229.5T ES13748229T ES2608860T3 ES 2608860 T3 ES2608860 T3 ES 2608860T3 ES 13748229 T ES13748229 T ES 13748229T ES 2608860 T3 ES2608860 T3 ES 2608860T3
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ES
Spain
Prior art keywords
compound
formula
salt
mixture
converting
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.)
Active
Application number
ES13748229.5T
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English (en)
Spanish (es)
Inventor
Dominika Pcion
Carrie TOMASI
Mark Charles WHITCOMB
Eric D. Dowdy
Wenyi FU
Patricia Macleod
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.)
Gilead Sciences Inc
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Gilead Sciences Inc
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.)
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Application filed by Gilead Sciences Inc filed Critical Gilead Sciences Inc
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Publication of ES2608860T3 publication Critical patent/ES2608860T3/es
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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C43/00Ethers; Compounds having groups, groups or groups
    • C07C43/02Ethers
    • C07C43/20Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring
    • C07C43/225Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring containing halogen
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C43/00Ethers; Compounds having groups, groups or groups
    • C07C43/02Ethers
    • C07C43/257Ethers having an ether-oxygen atom bound to carbon atoms both belonging to six-membered aromatic rings
    • C07C43/29Ethers having an ether-oxygen atom bound to carbon atoms both belonging to six-membered aromatic rings containing halogen
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/27Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by oxidation
    • C07C45/30Preparation 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/45Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by condensation
    • C07C45/46Friedel-Crafts reactions
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C49/00Ketones; Ketenes; Dimeric ketenes; Ketonic chelates
    • C07C49/76Ketones containing a keto group bound to a six-membered aromatic ring
    • C07C49/84Ketones containing a keto group bound to a six-membered aromatic ring containing ether groups, groups, groups, or groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C67/00Preparation of carboxylic acid esters
    • C07C67/12Preparation of carboxylic acid esters from asymmetrical anhydrides
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C67/00Preparation of carboxylic acid esters
    • C07C67/30Preparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group
    • C07C67/333Preparation 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
    • C07C67/343Preparation 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic 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
    • C07D215/16Heterocyclic 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
    • C07D215/48Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D215/54Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3
    • C07D215/56Carbon 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

Landscapes

  • 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)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Quinoline Compounds (AREA)
ES13748229.5T 2012-08-03 2013-08-01 Proceso e intermedios para preparar inhibidores de la integrasa Active ES2608860T3 (es)

Applications Claiming Priority (3)

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

Publications (1)

Publication Number Publication Date
ES2608860T3 true ES2608860T3 (es) 2017-04-17

Family

ID=48980354

Family Applications (1)

Application Number Title Priority Date Filing Date
ES13748229.5T Active ES2608860T3 (es) 2012-08-03 2013-08-01 Proceso e intermedios para preparar inhibidores de la integrasa

Country Status (17)

Country Link
US (1) US8877931B2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
EP (1) EP2880017B1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
JP (1) JP6147856B2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
KR (1) KR20150040340A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
CN (1) CN104520275B (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
AU (1) AU2013296289B2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
BR (1) BR112015002275A2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
CA (1) CA2878699C (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
EA (1) EA026089B1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
ES (1) ES2608860T3 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
IL (1) IL236618A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
IN (1) IN2015DN01688A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
MX (1) MX337094B (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
NZ (1) NZ630199A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
PT (1) PT2880017T (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
SG (1) SG11201500812QA (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
WO (1) WO2014022707A1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HUE028284T2 (en) 2012-12-21 2016-12-28 Gilead Sciences Inc Polycyclic carbamoylpyridone compounds and their pharmaceutical use
SMT201700498T1 (it) 2013-07-12 2017-11-15 Gilead Sciences Inc Composti di carbamoilpiridone policiclici e loro uso per il trattamento di infezioni da hiv
NO2865735T3 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html) 2013-07-12 2018-07-21
TWI677489B (zh) 2014-06-20 2019-11-21 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
NO2717902T3 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html) 2014-06-20 2018-06-23
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
TWI738321B (zh) 2014-12-23 2021-09-01 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
CN110790773A (zh) 2015-04-02 2020-02-14 吉利德科学公司 多环氨甲酰基吡啶酮化合物及其药物用途
CA3160068A1 (en) * 2019-09-24 2021-04-01 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

Family Cites Families (21)

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SE9904108D0 (sv) * 1999-11-15 1999-11-15 New Pharma Research Ab Nya föreningar
WO2002048113A1 (en) 2000-12-14 2002-06-20 The Procter & Gamble Company Cyclization process step in the making of quinolones and naphthyridines
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
PT1564210E (pt) 2002-11-20 2009-10-26 Japan Tobacco Inc Compostos de 4-oxoquinolina e a sua utilização como inibidores da integrase do hiv
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
JP4629104B2 (ja) 2004-05-21 2011-02-09 日本たばこ産業株式会社 4−オキソキノリン誘導体および抗hiv剤を含む併用剤
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
EP1992607B9 (en) 2006-03-06 2015-07-01 Japan Tobacco, Inc. Method for producing 4-oxoquinoline compound
IN2014CN00532A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html) 2006-03-06 2015-04-03 Japan Tobacco Inc
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
CA2661943C (en) 2006-09-12 2015-11-03 Gilead Sciences, Inc. Process and intermediates for preparing integrase inhibitors
US20100331331A1 (en) 2007-06-29 2010-12-30 Therapeutic Compositons And Use Thereof Therapeutic compositions and the use thereof
JP5547067B2 (ja) 2007-06-29 2014-07-09 ギリアード サイエンシーズ, インコーポレイテッド 治療組成物およびその使用
AR068403A1 (es) 2007-09-11 2009-11-18 Gilead Sciences Inc Proceso e intermediarios para la preparacion de inhibidores de integrasa

Also Published As

Publication number Publication date
EP2880017B1 (en) 2016-10-05
PT2880017T (pt) 2016-12-14
CN104520275A (zh) 2015-04-15
HK1209415A1 (en) 2016-04-01
JP6147856B2 (ja) 2017-06-14
MX337094B (es) 2016-02-10
KR20150040340A (ko) 2015-04-14
IL236618A (en) 2017-04-30
US20140039194A1 (en) 2014-02-06
EA201590018A1 (ru) 2015-05-29
IL236618A0 (en) 2015-02-26
AU2013296289A1 (en) 2015-02-19
CA2878699C (en) 2018-09-11
CA2878699A1 (en) 2014-02-06
BR112015002275A2 (pt) 2017-07-04
SG11201500812QA (en) 2015-04-29
AU2013296289B2 (en) 2017-10-05
IN2015DN01688A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html) 2015-07-03
CN104520275B (zh) 2016-11-02
HK1209748A1 (en) 2016-04-08
MX2015001506A (es) 2015-04-08
WO2014022707A1 (en) 2014-02-06
EP2880017A1 (en) 2015-06-10
EA026089B1 (ru) 2017-02-28
JP2015524822A (ja) 2015-08-27
NZ630199A (en) 2016-12-23
US8877931B2 (en) 2014-11-04

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