KR20150040340A - 인테그라아제 저해제 제조를 위한 방법 및 중간체 - Google Patents

인테그라아제 저해제 제조를 위한 방법 및 중간체 Download PDF

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Publication number
KR20150040340A
KR20150040340A KR20157005620A KR20157005620A KR20150040340A KR 20150040340 A KR20150040340 A KR 20150040340A KR 20157005620 A KR20157005620 A KR 20157005620A KR 20157005620 A KR20157005620 A KR 20157005620A KR 20150040340 A KR20150040340 A KR 20150040340A
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KR
South Korea
Prior art keywords
compound
formula
salt
mixture
rti
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.)
Abandoned
Application number
KR20157005620A
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English (en)
Korean (ko)
Inventor
도미니카 프키온
캐리 토마시
마크 찰스 위트콤
에릭 디 다우디
웬이 푸
패트리시아 매클라우드
Original Assignee
길리애드 사이언시즈, 인코포레이티드
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 길리애드 사이언시즈, 인코포레이티드 filed Critical 길리애드 사이언시즈, 인코포레이티드
Publication of KR20150040340A publication Critical patent/KR20150040340A/ko
Abandoned legal-status Critical Current

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Classifications

    • 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

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)
KR20157005620A 2012-08-03 2013-08-01 인테그라아제 저해제 제조를 위한 방법 및 중간체 Abandoned KR20150040340A (ko)

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 (1)

Publication Number Publication Date
KR20150040340A true KR20150040340A (ko) 2015-04-14

Family

ID=48980354

Family Applications (1)

Application Number Title Priority Date Filing Date
KR20157005620A Abandoned KR20150040340A (ko) 2012-08-03 2013-08-01 인테그라아제 저해제 제조를 위한 방법 및 중간체

Country Status (17)

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)

Families Citing this family (10)

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EA030003B1 (ru) 2012-12-21 2018-06-29 Джилид Сайэнс, Инк. Полициклическое карбамоилпиридоновое соединение и его фармацевтическое применение для лечения вич-инфекции
NO2865735T3 (enExample) 2013-07-12 2018-07-21
DK3019503T3 (da) 2013-07-12 2017-11-20 Gilead Sciences Inc Polycykliske-carbamoylpyridon-forbindelser og anvendelse deraf til behandling af hiv-infektioner
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
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
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
EP4036096A4 (en) * 2019-09-24 2023-08-09 Asymchem Laboratories (Tianjin) Co., Ltd. METHOD FOR THE CONTINUOUS PREPARATION OF ZINC BENZYL HALIDE AND ITS DERIVATIVES
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
HUP0303991A3 (en) 2000-12-14 2012-09-28 Warner Chilcott 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
US7176220B2 (en) 2002-11-20 2007-02-13 Japan Tobacco Inc. 4-oxoquinoline compound and use thereof as pharmaceutical agent
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
MY134672A (en) 2004-05-20 2007-12-31 Japan Tobacco Inc Stable crystal of 4-oxoquinoline compound
US7531554B2 (en) 2004-05-20 2009-05-12 Japan Tobacco Inc. 4-oxoquinoline compound and use thereof as HIV integrase inhibitor
US8633219B2 (en) 2004-05-21 2014-01-21 Japan Tobacco Inc. Combination therapy
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
CN101437801B (zh) 2006-03-06 2013-02-06 日本烟草产业株式会社 制备4-氧代喹啉化合物的方法
JP4669040B2 (ja) 2006-03-06 2011-04-13 日本たばこ産業株式会社 4−オキソキノリン化合物の製造方法
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
ES2536923T3 (es) 2006-09-12 2015-05-29 Gilead Sciences, Inc. Proceso e intermedios para preparar inhibidores de la integrasa del VIH
SG182229A1 (en) 2007-06-29 2012-07-30 Gilead Sciences Inc Therapeutic compositions and the use thereof
WO2009006203A1 (en) 2007-06-29 2009-01-08 Gilead Sciences, Inc. Therapeutic compositions and the use thereof
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
IL236618A (en) 2017-04-30
SG11201500812QA (en) 2015-04-29
CN104520275B (zh) 2016-11-02
EA026089B1 (ru) 2017-02-28
EP2880017B1 (en) 2016-10-05
JP6147856B2 (ja) 2017-06-14
NZ630199A (en) 2016-12-23
HK1209415A1 (en) 2016-04-01
WO2014022707A1 (en) 2014-02-06
MX2015001506A (es) 2015-04-08
CA2878699C (en) 2018-09-11
EP2880017A1 (en) 2015-06-10
US8877931B2 (en) 2014-11-04
ES2608860T3 (es) 2017-04-17
CA2878699A1 (en) 2014-02-06
EA201590018A1 (ru) 2015-05-29
IL236618A0 (en) 2015-02-26
IN2015DN01688A (enExample) 2015-07-03
BR112015002275A2 (pt) 2017-07-04
CN104520275A (zh) 2015-04-15
AU2013296289B2 (en) 2017-10-05
JP2015524822A (ja) 2015-08-27
AU2013296289A1 (en) 2015-02-19
PT2880017T (pt) 2016-12-14
HK1209748A1 (en) 2016-04-08
MX337094B (es) 2016-02-10
US20140039194A1 (en) 2014-02-06

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PA0105 International application

Patent event date: 20150303

Patent event code: PA01051R01D

Comment text: International Patent Application

PG1501 Laying open of application
A201 Request for examination
PA0201 Request for examination

Patent event code: PA02012R01D

Patent event date: 20180720

Comment text: Request for Examination of Application

E701 Decision to grant or registration of patent right
PE0701 Decision of registration

Patent event code: PE07011S01D

Comment text: Decision to Grant Registration

Patent event date: 20190816

NORF Unpaid initial registration fee
PC1904 Unpaid initial registration fee