WO2011102640A3 - Method for preparing sitagliptin and amine salt intermediates used therein - Google Patents

Method for preparing sitagliptin and amine salt intermediates used therein Download PDF

Info

Publication number
WO2011102640A3
WO2011102640A3 PCT/KR2011/001024 KR2011001024W WO2011102640A3 WO 2011102640 A3 WO2011102640 A3 WO 2011102640A3 KR 2011001024 W KR2011001024 W KR 2011001024W WO 2011102640 A3 WO2011102640 A3 WO 2011102640A3
Authority
WO
WIPO (PCT)
Prior art keywords
amine salt
intermediates used
preparing sitagliptin
salt intermediates
sitagliptin
Prior art date
Application number
PCT/KR2011/001024
Other languages
French (fr)
Other versions
WO2011102640A2 (en
Inventor
Ji-Yeon Chang
Hyun Seung Lee
Dong Jun Kim
Myoung-Sil Ko
Nam Du Kim
Young Kil Chang
Maeng Sup Kim
Original Assignee
Hanmi Holdings Co., 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 Hanmi Holdings Co., Ltd. filed Critical Hanmi Holdings Co., Ltd.
Publication of WO2011102640A2 publication Critical patent/WO2011102640A2/en
Publication of WO2011102640A3 publication Critical patent/WO2011102640A3/en

Links

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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

The present invention relates to a method for preparing sitagliptin by using an amine salt of (3R)-3-azido-4-(2,4,5-trifluorophenyl)-butyric acid (formula (V)) in a high yield and purity, and amine salt intermediates used therein.
PCT/KR2011/001024 2010-02-19 2011-02-16 Method for preparing sitagliptin and amine salt intermediates used therein WO2011102640A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
KR1020100015273A KR101156587B1 (en) 2010-02-19 2010-02-19 Preparation method of sitagliptin and amine salt intermediate used therein
KR10-2010-0015273 2010-02-19

Publications (2)

Publication Number Publication Date
WO2011102640A2 WO2011102640A2 (en) 2011-08-25
WO2011102640A3 true WO2011102640A3 (en) 2012-01-19

Family

ID=44483461

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/KR2011/001024 WO2011102640A2 (en) 2010-02-19 2011-02-16 Method for preparing sitagliptin and amine salt intermediates used therein

Country Status (2)

Country Link
KR (1) KR101156587B1 (en)
WO (1) WO2011102640A2 (en)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20130289276A1 (en) * 2010-10-08 2013-10-31 Cadila Healthcare Limited Process for preparing an intermediate of sitagliptin via enzymatic conversion
US20140336196A1 (en) * 2011-05-27 2014-11-13 Merck Sharp & Dohme Corp. Phosphoric acid salts of sitagliptin
EP2615080A1 (en) 2012-01-12 2013-07-17 LEK Pharmaceuticals d.d. Preparation of Optically Pure ß-Amino Acid Type Active Pharmaceutical Ingredients and Intermediates thereof
CZ2012111A3 (en) 2012-02-16 2013-08-28 Zentiva, K.S. Process for preparing rivaroxaban based on the use of (S)-epichlorohydrin
CN102627648B (en) * 2012-04-14 2014-11-12 江苏施美康药业股份有限公司 Preparation method of sitagliptin
CA2881050A1 (en) 2012-08-08 2014-02-13 Cipla Limited Process for the preparation of sitagliptin and intermediate compounds

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005003135A1 (en) * 2003-06-24 2005-01-13 Merck & Co., Inc. Phosphoric acid salt of a dipeptidyl peptidase-iv inhibitor
WO2007035198A2 (en) * 2005-07-25 2007-03-29 Merck & Co., Inc. Dodecylsulfate salt of a dipeptidyl peptidase-iv inhibitor
WO2011049344A2 (en) * 2009-10-21 2011-04-28 Hanmi Holdings Co., Ltd. Method of preparing sitagliptin and intermediates used therein

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA74912C2 (en) 2001-07-06 2006-02-15 Merck & Co Inc Beta-aminotetrahydroimidazo-(1,2-a)-pyrazines and tetratriazolo-(4,3-a)-pyrazines as inhibitors of dipeptylpeptidase for the treatment or prevention of diabetes
KR20070111099A (en) * 2006-05-16 2007-11-21 영진약품공업주식회사 Novel crystalline form of sitagliptin hydrochloride
KR101014885B1 (en) * 2008-07-09 2011-02-15 강원대학교산학협력단 Synthesis of allyl benzene derivatives using Pd and ligand

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005003135A1 (en) * 2003-06-24 2005-01-13 Merck & Co., Inc. Phosphoric acid salt of a dipeptidyl peptidase-iv inhibitor
WO2007035198A2 (en) * 2005-07-25 2007-03-29 Merck & Co., Inc. Dodecylsulfate salt of a dipeptidyl peptidase-iv inhibitor
WO2011049344A2 (en) * 2009-10-21 2011-04-28 Hanmi Holdings Co., Ltd. Method of preparing sitagliptin and intermediates used therein

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, 2005, pages 634 - 639 *
KIM, DOOSEOP ET AL.: "(2R)-4-0xo-4-[3-(Trifluoromethyl)-5,6-dihydro[1,2,4]tr iazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: A Pot ent, Orally Active Dipeptidyl Peptidase IV Inhibitor for the Treatment of T epe 2 Diabetes", J. MED. CHEM., vol. 48, 2005, pages 141 - 151 *

Also Published As

Publication number Publication date
WO2011102640A2 (en) 2011-08-25
KR20110095672A (en) 2011-08-25
KR101156587B1 (en) 2012-06-20

Similar Documents

Publication Publication Date Title
NZ600119A (en) Process and intermediates for the preparation of 5-biphenyl-4-yl-2-methylpentanoic acid derivatives
WO2012138147A3 (en) 1-(3-cyano-1-isopropyl-indol-5-yl)pyrazole-4-carboxylic acid crystalline form and the producing method thereof
WO2012103279A3 (en) Methods and compositions for the synthesis of multimerizing agents
WO2011087316A3 (en) Method for preparing tetrazole methanesulfonic acid salts, and novel compound used in same
WO2011102640A3 (en) Method for preparing sitagliptin and amine salt intermediates used therein
MX352470B (en) Malonic acid di-salts and a method for preparing malonyl dihalides.
WO2008096372A3 (en) Process for preparing highly pure ezetimibe using novel intermediates
MY150280A (en) Process of preparing derivatives of 1-(2-halobiphenyl-4-yl)-cyclopropanecarboxylic acid
MX2014014138A (en) New process for the preparation of 2-cyclopentyl-6-methoxy-isonic otinic acid.
MX2011009898A (en) Process for the preparation of propionic acid derivatives.
WO2010004578A3 (en) Novel and improved processes for the preparation of paliperidone
WO2012093411A3 (en) Process for the preparation of r-(-)-3- (carbamoylmethyl)-5-methylhexanoic acid and the intermediates
WO2012176214A3 (en) Process for bendamustine hydrochloride
WO2012112841A3 (en) [1,2,4]oxadiazol-3-yl acid salts and crystalline forms and their preparation
MX2010009926A (en) New process for the preparatiion of cyclohexanecarboxylic acid dericatives.
AP2007004270A0 (en) Process for preparing salts of hydrocyanic acid
MY164880A (en) Process for the preparation of isoxazolyl-methoxy-nicotinic acids
IN2014CN02346A (en)
MX2010009876A (en) New process for the preparation of cyclohexanecarboxylic acid derivatives via the corresponding cyclohexanecarboxamide derivative.
IN2014MN00971A (en)
AU2011300642A1 (en) Process for producing crystalline 5-aminosalicylic acid
WO2012044043A3 (en) Novel method of preparing benzoimidazole derivatives
WO2011007136A3 (en) Process for the preparation of o-desmethyl venlafaxine and intermediate for use therein
WO2009060297A3 (en) An improved process for the preparation of paliperidone and its intermediates
WO2009122429A3 (en) Crystalline oxybutynin and process for preparing the same

Legal Events

Date Code Title Description
121 Ep: the epo has been informed by wipo that ep was designated in this application

Ref document number: 11744882

Country of ref document: EP

Kind code of ref document: A2

NENP Non-entry into the national phase

Ref country code: DE

122 Ep: pct application non-entry in european phase

Ref document number: 11744882

Country of ref document: EP

Kind code of ref document: A2