WO2011004389A3 - An improved process for the preparation of elvitegravir - Google Patents

An improved process for the preparation of elvitegravir Download PDF

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Publication number
WO2011004389A3
WO2011004389A3 PCT/IN2010/000420 IN2010000420W WO2011004389A3 WO 2011004389 A3 WO2011004389 A3 WO 2011004389A3 IN 2010000420 W IN2010000420 W IN 2010000420W WO 2011004389 A3 WO2011004389 A3 WO 2011004389A3
Authority
WO
WIPO (PCT)
Prior art keywords
formula
compound
elvitegravir
preparation
improved process
Prior art date
Application number
PCT/IN2010/000420
Other languages
French (fr)
Other versions
WO2011004389A2 (en
Inventor
Siva Rama Prasad Vellanki
Vilas Nathu Dhake
Satyanarayana Ravi
Ravi Nuchu
Ravindra Puliyala
Mahaboob Basha Shaik
Debashish Datta
Original Assignee
Matrix Laboratories Ltd
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 Matrix Laboratories Ltd filed Critical Matrix Laboratories Ltd
Publication of WO2011004389A2 publication Critical patent/WO2011004389A2/en
Publication of WO2011004389A3 publication Critical patent/WO2011004389A3/en

Links

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
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
    • C07D215/233—Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)

Abstract

The present invention relates to improved process for the preparation of elvitegravir (12), wherein the compound of formula (6) is protected with suitable protecting agents and further reacted with formula (9) in the presence of tetrakis(triphenylphosphine)-palladium (0) catalyst in tetrahydofuran to get corresponding condensed products, which are subjected to hydrolysis, de-protection to get compound of formula (11). The compound of formula (11) is optionally treated with amine to get amine addition salt of formula (11D), then setting free of amine salt in the presence of acid to get pure compound of formula (11). The pure compound of formula (11) is reacted with sodium alkoxide to get pure elvitegravir (12).
PCT/IN2010/000420 2009-06-18 2010-06-18 An improved process for the preparation of elvitegravir WO2011004389A2 (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
IN1435CH2009 2009-06-18
IN1435/CHE/2009 2009-06-18
IN2558/CHE/2009 2009-10-23
IN2558CH2009 2009-10-23

Publications (2)

Publication Number Publication Date
WO2011004389A2 WO2011004389A2 (en) 2011-01-13
WO2011004389A3 true WO2011004389A3 (en) 2011-04-28

Family

ID=43242452

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IN2010/000420 WO2011004389A2 (en) 2009-06-18 2010-06-18 An improved process for the preparation of elvitegravir

Country Status (1)

Country Link
WO (1) WO2011004389A2 (en)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CZ304983B6 (en) 2012-10-12 2015-03-11 Zentiva, K.S. Preparation process and novel intermediates of elvitegravir synthesis
CZ304984B6 (en) 2012-10-12 2015-03-11 Zentiva, K.S. Enhanced process for preparing and novel intermediates of elvitegravir synthesis
CN103819402B (en) * 2012-11-17 2016-03-30 上海迪赛诺化学制药有限公司 Dust is for drawing Wei intermediate and its preparation method and application
CZ307255B6 (en) * 2013-07-11 2018-05-02 Zentiva, K.S. A new method of preparing elvitegravir
CN105315203A (en) * 2014-06-06 2016-02-10 上海迪赛诺化学制药有限公司 V-type elvitegravir crystal and preparation method thereof
WO2016193997A2 (en) * 2015-06-03 2016-12-08 Msn Laboratories Private Limited Process for the preparation of 6-(3-chloro-2-fluorobenzyl)-1-[(2s)-1-hydroxy-3-methylbutan-2-yl]-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid and pharmaceutically acceptable salts thereof
CN106008195B (en) * 2016-05-19 2018-08-03 绍兴文理学院 The preparation method of 2,4- of one kind, bis- fluoro- 5- iodo-benzoic acids

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005113508A1 (en) * 2004-05-20 2005-12-01 Japan Tobacco Inc. Stable crystal of 4-oxoquinoline compound
US7176220B2 (en) * 2002-11-20 2007-02-13 Japan Tobacco Inc. 4-oxoquinoline compound and use thereof as pharmaceutical agent
WO2007102499A1 (en) * 2006-03-06 2007-09-13 Japan Tobacco Inc. Process for production of 4-oxoquinoline compound

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6248736B1 (en) 1999-01-08 2001-06-19 Pharmacia & Upjohn Company 4-oxo-1,4-dihydro-3-quinolinecarboxamides as antiviral agents
US6248739B1 (en) 1999-01-08 2001-06-19 Pharmacia & Upjohn Company Quinolinecarboxamides as antiviral agents
PE20011349A1 (en) 2000-06-16 2002-01-19 Upjohn Co 1-ARIL-4-OXO-1,4-DIHYDRO-3-QUINOLINE CARBOXAMIDES AS ANTIVIRAL AGENTS
AR068403A1 (en) 2007-09-11 2009-11-18 Gilead Sciences Inc PROCESS AND INTERMEDIARIES FOR THE PREPARATION OF INTEGRASA INHIBITORS

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7176220B2 (en) * 2002-11-20 2007-02-13 Japan Tobacco Inc. 4-oxoquinoline compound and use thereof as pharmaceutical agent
WO2005113508A1 (en) * 2004-05-20 2005-12-01 Japan Tobacco Inc. Stable crystal of 4-oxoquinoline compound
WO2007102499A1 (en) * 2006-03-06 2007-09-13 Japan Tobacco Inc. Process for production of 4-oxoquinoline compound
US20090318702A1 (en) * 2006-03-06 2009-12-24 Koji Matsuda Process for production of 4-oxoquinoline compound

Also Published As

Publication number Publication date
WO2011004389A2 (en) 2011-01-13

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