AU2013296289B2 - Process and intermediates for preparing integrase inhibitors - Google Patents

Process and intermediates for preparing integrase inhibitors Download PDF

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Publication number
AU2013296289B2
AU2013296289B2 AU2013296289A AU2013296289A AU2013296289B2 AU 2013296289 B2 AU2013296289 B2 AU 2013296289B2 AU 2013296289 A AU2013296289 A AU 2013296289A AU 2013296289 A AU2013296289 A AU 2013296289A AU 2013296289 B2 AU2013296289 B2 AU 2013296289B2
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AU
Australia
Prior art keywords
compound
formula
salt
mixture
converting
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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.)
Ceased
Application number
AU2013296289A
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English (en)
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AU2013296289A1 (en
Inventor
Eric D. Dowdy
Wenyi FU
Patricia Macleod
Dominika Pcion
Carrie TOMASI
Mark Charles Whitcomb
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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Publication date
Application filed by Gilead Sciences Inc filed Critical Gilead Sciences Inc
Publication of AU2013296289A1 publication Critical patent/AU2013296289A1/en
Application granted granted Critical
Publication of AU2013296289B2 publication Critical patent/AU2013296289B2/en
Ceased legal-status Critical Current
Anticipated expiration legal-status Critical

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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

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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)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Quinoline Compounds (AREA)
AU2013296289A 2012-08-03 2013-08-01 Process and intermediates for preparing integrase inhibitors Ceased AU2013296289B2 (en)

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
AU2013296289A1 AU2013296289A1 (en) 2015-02-19
AU2013296289B2 true AU2013296289B2 (en) 2017-10-05

Family

ID=48980354

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2013296289A Ceased AU2013296289B2 (en) 2012-08-03 2013-08-01 Process and intermediates for preparing integrase inhibitors

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)

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PL2822954T3 (pl) 2012-12-21 2016-09-30 Policykliczne związki karbamoilopirydonu i ich farmaceutyczne zastosowanie
NO2865735T3 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html) 2013-07-12 2018-07-21
EP3019503B1 (en) 2013-07-12 2017-09-06 Gilead Sciences, Inc. Polycyclic-carbamoylpyridone compounds and their use for the treatment of hiv infections
NO2717902T3 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html) 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
NZ735575A (en) 2015-04-02 2018-11-30 Gilead Sciences Inc Polycyclic-carbamoylpyridone compounds and their pharmaceutical use
EP4036096A4 (en) * 2019-09-24 2023-08-09 Asymchem Laboratories (Tianjin) Co., Ltd. CONTINUOUS MANUFACTURING PROCESS FOR BENZYLZINC HALIDE AND DERIVATIVES 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

Citations (1)

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WO2009036161A1 (en) * 2007-09-11 2009-03-19 Gilead Sciences, Inc. Process and intermediates for preparing integrase inhibitors

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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
BRPI0708685B8 (pt) 2006-03-06 2021-05-25 Japan Tobacco Inc composto de 4-oxoquinolina, seu uso e método para produção dos mesmos
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Also Published As

Publication number Publication date
EP2880017A1 (en) 2015-06-10
MX2015001506A (es) 2015-04-08
HK1209748A1 (en) 2016-04-08
JP6147856B2 (ja) 2017-06-14
IN2015DN01688A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html) 2015-07-03
IL236618A0 (en) 2015-02-26
JP2015524822A (ja) 2015-08-27
WO2014022707A1 (en) 2014-02-06
AU2013296289A1 (en) 2015-02-19
EP2880017B1 (en) 2016-10-05
CA2878699C (en) 2018-09-11
CN104520275A (zh) 2015-04-15
BR112015002275A2 (pt) 2017-07-04
CN104520275B (zh) 2016-11-02
NZ630199A (en) 2016-12-23
IL236618A (en) 2017-04-30
US20140039194A1 (en) 2014-02-06
KR20150040340A (ko) 2015-04-14
ES2608860T3 (es) 2017-04-17
US8877931B2 (en) 2014-11-04
EA201590018A1 (ru) 2015-05-29
MX337094B (es) 2016-02-10
CA2878699A1 (en) 2014-02-06
SG11201500812QA (en) 2015-04-29
EA026089B1 (ru) 2017-02-28
HK1209415A1 (en) 2016-04-01
PT2880017T (pt) 2016-12-14

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MK14 Patent ceased section 143(a) (annual fees not paid) or expired