WO2012042534A3 - Preparation of r-sitagliptin and intermediates thereof - Google Patents

Preparation of r-sitagliptin and intermediates thereof Download PDF

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Publication number
WO2012042534A3
WO2012042534A3 PCT/IN2011/000649 IN2011000649W WO2012042534A3 WO 2012042534 A3 WO2012042534 A3 WO 2012042534A3 IN 2011000649 W IN2011000649 W IN 2011000649W WO 2012042534 A3 WO2012042534 A3 WO 2012042534A3
Authority
WO
WIPO (PCT)
Prior art keywords
sitagliptin
preparation
intermediates
compound
formula
Prior art date
Application number
PCT/IN2011/000649
Other languages
French (fr)
Other versions
WO2012042534A2 (en
Inventor
Santosh Badgujar
Milind Moreshwar Gharpure
Roop Singh Yadav
Original Assignee
Glenmark Generics Limited
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 Glenmark Generics Limited filed Critical Glenmark Generics Limited
Publication of WO2012042534A2 publication Critical patent/WO2012042534A2/en
Publication of WO2012042534A3 publication Critical patent/WO2012042534A3/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C227/00—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C227/12—Formation of amino and carboxyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C239/00—Compounds containing nitrogen-to-halogen bonds; Hydroxylamino compounds or ethers or esters thereof
    • C07C239/08—Hydroxylamino compounds or their ethers or esters
    • C07C239/18—Hydroxylamino compounds or their ethers or esters having nitrogen atoms of hydroxylamino groups further bound to carbon atoms of hydrocarbon radicals substituted by carboxyl groups

Abstract

Provided is preparation method of R-sitagliptin. Compound of formula (IV), amine salt thereof and method for preparation thereof are also provided. Said compound of formula (IV) or amine salt thereof is useful as key intermediate in the synthesis of R-sitagliptin or pharmaceutically acceptable salts thereof.
PCT/IN2011/000649 2010-09-28 2011-09-21 Processes for the preparation of r-sitagliptin and intermediates thereof WO2012042534A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN2698MU2010 2010-09-28
IN2698/MUM/2010 2010-09-28

Publications (2)

Publication Number Publication Date
WO2012042534A2 WO2012042534A2 (en) 2012-04-05
WO2012042534A3 true WO2012042534A3 (en) 2012-06-07

Family

ID=45893593

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IN2011/000649 WO2012042534A2 (en) 2010-09-28 2011-09-21 Processes for the preparation of r-sitagliptin and intermediates thereof

Country Status (1)

Country Link
WO (1) WO2012042534A2 (en)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9453042B2 (en) 2007-10-25 2016-09-27 Cempra Pharmaceuticals, Inc. Process for the preparation of macrolide antibacterial agents
AU2009308182B2 (en) 2008-10-24 2016-05-19 Cempra Pharmaceuticals, Inc. Biodefenses using triazole-containing macrolides
US9937194B1 (en) 2009-06-12 2018-04-10 Cempra Pharmaceuticals, Inc. Compounds and methods for treating inflammatory diseases
EP2475253B1 (en) 2009-09-10 2016-10-26 Cempra Pharmaceuticals, Inc. Methods for treating malaria, tuberculosis and mac diseases
KR20130120458A (en) 2010-09-10 2013-11-04 셈프라 파마슈티컬스, 인크. Hydrogen bond forming fluoro ketolides for treating diseases
US10188674B2 (en) 2012-03-27 2019-01-29 Cempra Pharmaceuticals, Inc. Parenteral formulations for administering macrolide antibiotics
US9233967B2 (en) 2012-08-08 2016-01-12 Cipla Limited Process for the preparation of sitagliptin and intermediate compounds
CA2905975A1 (en) 2013-03-14 2014-09-25 Cempra Pharmaceuticals, Inc. Methods for treating respiratory diseases and formulations therefor
CN105188712A (en) 2013-03-15 2015-12-23 森普拉制药公司 Convergent processes for preparing macrolide antibacterial agents
CN103232455A (en) * 2013-05-14 2013-08-07 聊城九州和谷生物科技有限公司 Industrial production method of sitagliptin
WO2016127023A1 (en) * 2015-02-06 2016-08-11 Cempra Pharmaceuticals, Inc. 4-azidobutylamines and processes for preparing
CN107312010A (en) * 2017-08-14 2017-11-03 苏州信恩医药科技有限公司 Application of the trona in sitagliptin synthesis
CN113461691A (en) * 2020-12-31 2021-10-01 浙江美诺华药物化学有限公司 Sitagliptin impurity, preparation method and detection method thereof

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004085378A1 (en) * 2003-03-19 2004-10-07 Merck & Co. Inc. Process for the preparation of chiral beta amino acid derivatives by asymmetric hydrogenation
WO2004087650A2 (en) * 2003-03-27 2004-10-14 Merck & Co. Inc. Process and intermediates for the preparation of beta-amino acid amide dipeptidyl peptidase-iv inhibitors

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004085378A1 (en) * 2003-03-19 2004-10-07 Merck & Co. Inc. Process for the preparation of chiral beta amino acid derivatives by asymmetric hydrogenation
WO2004087650A2 (en) * 2003-03-27 2004-10-14 Merck & Co. Inc. Process and intermediates for the preparation of beta-amino acid amide dipeptidyl peptidase-iv inhibitors

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
HANSEN, KARL B. ET AL.: "First Generation Process for the Preparation of the DPP-IV Inhibitor Sitagliptin.", ORGANIC PROCESS RESEARCH & DEVELOPMENT., vol. 9, no. 5, 31 August 2005 (2005-08-31), pages 634 - 639, XP009142089, DOI: doi:10.1021/op0500786 *
ZHU, YANYUN. ET AL.: "Synthesis, biological assay in vitro and molecular docking studies of new imidazopyrazinone derivatives as potential dipeptidyl peptidase IV inhibitors.", EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 45, no. 11, 12 August 2010 (2010-08-12), pages 4953 - 4962, XP027408906 *

Also Published As

Publication number Publication date
WO2012042534A2 (en) 2012-04-05

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