WO2009065872A3 - Processes for the synthesis of varenicline l-tartrate - Google Patents

Processes for the synthesis of varenicline l-tartrate Download PDF

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Publication number
WO2009065872A3
WO2009065872A3 PCT/EP2008/065866 EP2008065866W WO2009065872A3 WO 2009065872 A3 WO2009065872 A3 WO 2009065872A3 EP 2008065866 W EP2008065866 W EP 2008065866W WO 2009065872 A3 WO2009065872 A3 WO 2009065872A3
Authority
WO
WIPO (PCT)
Prior art keywords
varenicline
tartrate
synthesis
processes
provides
Prior art date
Application number
PCT/EP2008/065866
Other languages
French (fr)
Other versions
WO2009065872A2 (en
Inventor
Stephen Winter
Luis Botella
Carmen NÁJERA
José SOTO
Original Assignee
Medichem, S.A.
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 Medichem, S.A. filed Critical Medichem, S.A.
Publication of WO2009065872A2 publication Critical patent/WO2009065872A2/en
Publication of WO2009065872A3 publication Critical patent/WO2009065872A3/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/08—Bridged systems

Abstract

This invention provides a process of preparing varenicline L-tartrate salt. This invention also provides varenicline L-tartrate produced by the instant method, as well as a pharmaceutical composition comprising same.
PCT/EP2008/065866 2007-11-20 2008-11-19 Improved processes for the synthesis of varenicline l-tartrate WO2009065872A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US374607P 2007-11-20 2007-11-20
US61/003,746 2007-11-20

Publications (2)

Publication Number Publication Date
WO2009065872A2 WO2009065872A2 (en) 2009-05-28
WO2009065872A3 true WO2009065872A3 (en) 2009-11-05

Family

ID=40289310

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2008/065866 WO2009065872A2 (en) 2007-11-20 2008-11-19 Improved processes for the synthesis of varenicline l-tartrate

Country Status (2)

Country Link
AR (1) AR071443A1 (en)
WO (1) WO2009065872A2 (en)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2268639A2 (en) 2008-05-22 2011-01-05 Teva Pharmaceutical Industries Ltd. Varenicline tosylate, an intermediate in the preparation process of varenicline l-tartrate
US20100010221A1 (en) * 2008-07-10 2010-01-14 Revital Lifshitz-Liron Processes for purifying varenicline l-tartrate salt and preparing crystalline forms of varenicline l-tartrate salt
US8178537B2 (en) 2009-06-22 2012-05-15 Teva Pharmaceutical Industries Ltd. Solid state forms of varenicline salts and processes for preparation thereof
WO2011110954A1 (en) * 2010-03-09 2011-09-15 Actavis Group Ptc Ehf Highly pure varenicline or a pharmaceutically acceptable salt thereof substantially free of methylvarenicline impurity
US20120004239A1 (en) * 2010-06-11 2012-01-05 Medichem, S.A. Process for Preparing Quinoxaline Derivatives
WO2018163190A1 (en) * 2017-03-08 2018-09-13 Jubilant Generics Limited (Formerly A Division Of Jubilant Lifesciences Limited) An improved process for the preparation of varenicline and salt thereof
CN113956255A (en) * 2020-07-20 2022-01-21 威智医药有限公司 Preparation method of varenicline intermediate, varenicline and salt thereof

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001062736A1 (en) * 2000-02-25 2001-08-30 Pfizer Products Inc. Aryl fused azapolycyclic compounds
WO2002085843A2 (en) * 2001-04-20 2002-10-31 Pfizer Products Inc. Process for the preparation of 1,3-substituted indenes and aryl-fused azapolycyclic compounds
WO2006090236A1 (en) * 2005-02-24 2006-08-31 Pfizer Products Inc. Preparation of high purity substituted quinoxaline
WO2008060487A2 (en) * 2006-11-09 2008-05-22 Pfizer Products Inc. Polymorphs of nicotinic intermediates

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001062736A1 (en) * 2000-02-25 2001-08-30 Pfizer Products Inc. Aryl fused azapolycyclic compounds
WO2002085843A2 (en) * 2001-04-20 2002-10-31 Pfizer Products Inc. Process for the preparation of 1,3-substituted indenes and aryl-fused azapolycyclic compounds
WO2006090236A1 (en) * 2005-02-24 2006-08-31 Pfizer Products Inc. Preparation of high purity substituted quinoxaline
WO2008060487A2 (en) * 2006-11-09 2008-05-22 Pfizer Products Inc. Polymorphs of nicotinic intermediates

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
COE J W ET AL: "Varenicline: an alpha4beta2 Nicotinic Receptor Partial Agonist for Smoking Cessation", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY, WASHINGTON., US, vol. 48, no. 10, 1 January 2005 (2005-01-01), pages 3474 - 3477, XP002474642, ISSN: 0022-2623 *

Also Published As

Publication number Publication date
WO2009065872A2 (en) 2009-05-28
AR071443A1 (en) 2010-06-23

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