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SG11201500812QA - Process and intermediates for preparing integrase inhibitors - Google Patents

Process and intermediates for preparing integrase inhibitors

Info

Publication number
SG11201500812QA
SG11201500812QA SG11201500812QA SG11201500812QA SG11201500812QA SG 11201500812Q A SG11201500812Q A SG 11201500812QA SG 11201500812Q A SG11201500812Q A SG 11201500812QA SG 11201500812Q A SG11201500812Q A SG 11201500812QA SG 11201500812Q A SG11201500812Q A SG 11201500812QA
Authority
SG
Singapore
Prior art keywords
intermediates
integrase inhibitors
preparing integrase
preparing
inhibitors
Prior art date
Application number
SG11201500812QA
Other languages
English (en)
Inventor
Dominika Pcion
Carrie Tomasi
Mark Charles Whitcomb
Eric D Dowdy
Wenyi Fu
Patricia Macleod
Original Assignee
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.)
Filing date
Publication date
Application filed by Gilead Sciences Inc filed Critical Gilead Sciences Inc
Publication of SG11201500812QA publication Critical patent/SG11201500812QA/en

Links

Classifications

    • 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
    • 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
    • C07C43/257—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

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)
  • Quinoline Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
SG11201500812QA 2012-08-03 2013-08-01 Process and intermediates for preparing integrase inhibitors SG11201500812QA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201261679475P 2012-08-03 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
SG11201500812QA true SG11201500812QA (en) 2015-04-29

Family

ID=48980354

Family Applications (1)

Application Number Title Priority Date Filing Date
SG11201500812QA SG11201500812QA (en) 2012-08-03 2013-08-01 Process and intermediates for preparing integrase inhibitors

Country Status (18)

Country Link
US (1) US8877931B2 (ja)
EP (1) EP2880017B1 (ja)
JP (1) JP6147856B2 (ja)
KR (1) KR20150040340A (ja)
CN (1) CN104520275B (ja)
AU (1) AU2013296289B2 (ja)
BR (1) BR112015002275A2 (ja)
CA (1) CA2878699C (ja)
EA (1) EA026089B1 (ja)
ES (1) ES2608860T3 (ja)
HK (2) HK1209415A1 (ja)
IL (1) IL236618A (ja)
IN (1) IN2015DN01688A (ja)
MX (1) MX337094B (ja)
NZ (1) NZ630199A (ja)
PT (1) PT2880017T (ja)
SG (1) SG11201500812QA (ja)
WO (1) WO2014022707A1 (ja)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA123572C2 (uk) 2012-12-21 2021-04-28 Гіліад Сайєнсіз, Інк. Поліциклічні карбамоїлпіридонові сполуки та їх фармацевтичне застосування
NO2865735T3 (ja) 2013-07-12 2018-07-21
AU2014286993B2 (en) 2013-07-12 2018-10-25 Gilead Sciences, Inc. Polycyclic-carbamoylpyridone compounds and their use for the treatment of HIV infections
NO2717902T3 (ja) 2014-06-20 2018-06-23
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
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
EP3466490B1 (en) 2015-04-02 2020-10-21 Gilead Sciences, Inc. Polycyclic-carbamoylpyridone compounds and their pharmaceutical use
WO2021056193A1 (zh) * 2019-09-24 2021-04-01 凯莱英医药集团（天津）股份有限公司 一种苄基卤化锌及其衍生物的连续制备方法
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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SE9904108D0 (sv) * 1999-11-15 1999-11-15 New Pharma Research Ab Nya föreningar
EP1343766B1 (en) 2000-12-14 2005-07-27 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
US20050104233A1 (en) 2002-05-31 2005-05-19 Shinji Kato 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
WO2004046115A1 (ja) 2002-11-20 2004-06-03 Japan Tobacco Inc. ４−オキソキノリン化合物及びそのｈｉｖインテグラーゼ阻害剤としての利用
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
US7531554B2 (en) 2004-05-20 2009-05-12 Japan Tobacco Inc. 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
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
BRPI0708685B8 (pt) 2006-03-06 2021-05-25 Japan Tobacco Inc composto de 4-oxoquinolina, seu uso e método para produção dos mesmos
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
CN101516819B (zh) 2006-09-12 2013-10-16 吉里德科学公司 制备整合酶抑制剂的方法和中间体
US20110009411A1 (en) 2007-06-29 2011-01-13 Gilead Sciences ,Inc. Therapeutic compositions and the use thereof
CN101686972B (zh) 2007-06-29 2013-08-14 吉里德科学公司 治疗用组合物和方法
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
CA2878699A1 (en) 2014-02-06
WO2014022707A1 (en) 2014-02-06
EA026089B1 (ru) 2017-02-28
CN104520275A (zh) 2015-04-15
EA201590018A1 (ru) 2015-05-29
ES2608860T3 (es) 2017-04-17
AU2013296289A1 (en) 2015-02-19
IL236618A (en) 2017-04-30
HK1209748A1 (en) 2016-04-08
IN2015DN01688A (ja) 2015-07-03
KR20150040340A (ko) 2015-04-14
HK1209415A1 (en) 2016-04-01
JP6147856B2 (ja) 2017-06-14
EP2880017A1 (en) 2015-06-10
CN104520275B (zh) 2016-11-02
BR112015002275A2 (pt) 2017-07-04
JP2015524822A (ja) 2015-08-27
CA2878699C (en) 2018-09-11
NZ630199A (en) 2016-12-23
EP2880017B1 (en) 2016-10-05
US20140039194A1 (en) 2014-02-06
PT2880017T (pt) 2016-12-14
MX337094B (es) 2016-02-10
US8877931B2 (en) 2014-11-04
AU2013296289B2 (en) 2017-10-05
MX2015001506A (es) 2015-04-08
IL236618A0 (en) 2015-02-26

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