WO2010122578A3 - Process for preparation of sitagliptin and its intermediates - Google Patents

Process for preparation of sitagliptin and its intermediates Download PDF

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Publication number
WO2010122578A3
WO2010122578A3 PCT/IN2010/000249 IN2010000249W WO2010122578A3 WO 2010122578 A3 WO2010122578 A3 WO 2010122578A3 IN 2010000249 W IN2010000249 W IN 2010000249W WO 2010122578 A3 WO2010122578 A3 WO 2010122578A3
Authority
WO
WIPO (PCT)
Prior art keywords
intermediates
preparation
sitagliptin
formula
improved processes
Prior art date
Application number
PCT/IN2010/000249
Other languages
French (fr)
Other versions
WO2010122578A2 (en
Inventor
Manne Satyanarayana Reddy
Sajja Eswaraiah
Revu Satyanarayana
Bairy Kondal Reddy
Aluru Srinivas
Original Assignee
Msn Laboratories 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 Msn Laboratories Limited filed Critical Msn Laboratories Limited
Publication of WO2010122578A2 publication Critical patent/WO2010122578A2/en
Publication of WO2010122578A3 publication Critical patent/WO2010122578A3/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/44—Iso-indoles; Hydrogenated iso-indoles
    • C07D209/48—Iso-indoles; Hydrogenated iso-indoles with oxygen atoms in positions 1 and 3, e.g. phthalimide
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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)
  • Health & Medical Sciences (AREA)
  • Diabetes (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

Improved processes for the preparation of Sitagliptin compound of formula-1 and its intermediates are provided.
PCT/IN2010/000249 2009-04-20 2010-04-20 Process for the preparation of sitagliptin and its intermediates WO2010122578A2 (en)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
IN901CH2009 2009-04-20
IN901/CHE/2009 2009-04-20
IN2652/CHE/2009 2009-11-03
IN2652CH2009 2009-11-03
IN1084CH2010 2010-04-19
IN1084/CHE/2010 2010-04-19

Publications (2)

Publication Number Publication Date
WO2010122578A2 WO2010122578A2 (en) 2010-10-28
WO2010122578A3 true WO2010122578A3 (en) 2010-12-29

Family

ID=43011552

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IN2010/000249 WO2010122578A2 (en) 2009-04-20 2010-04-20 Process for the preparation of sitagliptin and its intermediates

Country Status (1)

Country Link
WO (1) WO2010122578A2 (en)

Families Citing this family (47)

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KR101222679B1 (en) * 2009-10-21 2013-01-16 한미사이언스 주식회사 Method of preparing sitagliptin and intermediates used therein
US20130289276A1 (en) * 2010-10-08 2013-10-31 Cadila Healthcare Limited Process for preparing an intermediate of sitagliptin via enzymatic conversion
AU2011327903A1 (en) * 2010-11-11 2013-05-02 Redx Pharma Plc Drug derivatives
SI2691083T1 (en) 2011-03-29 2017-12-29 Krka, D.D., Novo Mesto Pharmaceutical composition of sitagliptin
EP2508506A1 (en) 2011-04-08 2012-10-10 LEK Pharmaceuticals d.d. Preparation of sitagliptin intermediates
CN102757431B (en) * 2011-04-24 2016-03-30 浙江华海药业股份有限公司 A kind of novel method of synthesizing sitagliptin
ITMI20110765A1 (en) * 2011-05-05 2012-11-06 Chemo Iberica Sa PROCESS FOR SITAGLIPTINA PRODUCTION
EP2527320A1 (en) 2011-05-27 2012-11-28 LEK Pharmaceuticals d.d. Preparation of Sitagliptin Intermediates
CN102838603B (en) * 2011-06-24 2015-05-13 上海医药工业研究院 Preparation method of intermediate compound of sitagliptin
EP2726484A1 (en) 2011-06-29 2014-05-07 Ranbaxy Laboratories Limited Solid dispersions of sitagliptin and processes for their preparation
EP2726483A1 (en) 2011-06-30 2014-05-07 Ranbaxy Laboratories Limited Novel salts of sitagliptin
SI2736909T1 (en) 2011-07-27 2017-08-31 Farma Grs, D.O.O. Process for the preparation of sitagliptin and its pharmaceutically acceptable salts
CN102391142B (en) * 2011-09-30 2013-08-07 山东铂源药业有限公司 Method for recycling 3-(S)-amino-4-(2,4,5-trifluoro-phenyl)-butyrate
CN102503829B (en) * 2011-10-08 2013-11-06 山东铂源药业有限公司 Preparation methods for sitagliptin intermediates
WO2013065066A1 (en) 2011-11-02 2013-05-10 Cadila Healthcare Limited Processes for preparing 4-oxo-4-[3-(trifluoromethyl)-5,6- dihydro [l,2,41-triazolo[43-a]pyrazin-7(8h)-yl]-l-(2,4,5- trifluorophenyl)butan-2-amine
WO2013084210A1 (en) 2011-12-08 2013-06-13 Ranbaxy Laboratories Limited Amorphous form of sitagliptin salts
CN103172539B (en) * 2011-12-23 2016-08-03 上海阳帆医药科技有限公司 The preparation method of Glucovance sitagliptin intermediate aminobenzene butyric acid derivative
EP2674432A1 (en) 2012-06-14 2013-12-18 LEK Pharmaceuticals d.d. New synthetic route for the preparation of ß aminobutyryl substituted 5,6,7,8-tetrahydro[1,4]diazolo[4,3-alpha]pyrazin-7-yl compounds
CA2881050A1 (en) 2012-08-08 2014-02-13 Cipla Limited Process for the preparation of sitagliptin and intermediate compounds
IN2013MU00916A (en) 2013-03-20 2015-06-26 Cadila Healthcare Ltd
CN104447374B (en) * 2013-09-17 2016-08-17 深圳翰宇药业股份有限公司 A kind of sitagliptin and the preparation method of intermediate thereof
CN103694245A (en) * 2014-01-14 2014-04-02 李友香 Crude medicine for hypoglycemic medicine
CN103709170A (en) * 2014-01-14 2014-04-09 李友香 Medicinal crude drug for reducing blood sugar
IN2014MU00212A (en) 2014-01-21 2015-08-28 Cadila Healthcare Ltd
WO2015120111A2 (en) * 2014-02-05 2015-08-13 Stereokem, Inc. (Usa) Expedient synthesis of sitagliptin
WO2015145333A1 (en) 2014-03-26 2015-10-01 Sun Pharmaceutical Industries Limited Process for the preparation of sitagliptin and its intermediate
WO2015189862A1 (en) * 2014-06-10 2015-12-17 Council Of Scientific & Industrial Research Chiral amines, a process for preparation and use thereof
CN104130149B (en) * 2014-07-18 2016-01-27 浙江昌明药业有限公司 A kind of recoverying and utilizing method of 3-(S)-amino butyric acid derivative
CN104130264B (en) * 2014-08-14 2016-08-31 广东东阳光药业有限公司 A kind of method for transformation of isomer
CN104387393A (en) * 2014-10-31 2015-03-04 广东东阳光药业有限公司 Preparation method of sitagliptin impurity
BR112017014856A2 (en) * 2015-01-08 2018-02-06 Lee Pharma Ltd innovative process for preparation of dipeptidyl peptidase-4 enzyme inhibitor (dpp-4)
CN105017081B (en) * 2015-07-08 2017-03-08 和鼎（南京）医药技术有限公司 A kind of preparation method of sitagliptin intermediate
CN105085531B (en) * 2015-09-06 2017-11-17 合肥华方医药科技有限公司 A kind of Xi Gelieting impurity synthetic method
CN105218371A (en) * 2015-09-24 2016-01-06 上海交通大学 The preparation method of optically pure 3-hydroxyl-4-(2,4,5-trifluorophenyl) ethyl butyrate
CN105130999B (en) * 2015-10-15 2017-10-20 合肥华方医药科技有限公司 A kind of synthetic method of Xi Gelieting impurity
CN105331651B (en) * 2015-11-25 2018-11-13 尚科生物医药（上海）有限公司 The enzyme-chemically preparation method of sitagliptin and its intermediate
US10047094B1 (en) * 2017-02-10 2018-08-14 F.I.S.—Fabbrica Italiana Sintetici S.p.A. Process for the preparation of triazole and salt thereof
CN107311862B (en) * 2017-06-19 2020-06-19 南京红杉生物科技有限公司 Preparation method of sitagliptin intermediate
CN109867659A (en) * 2017-12-04 2019-06-11 江苏恒瑞医药股份有限公司 The preparation method of benzo piperidine derivatives
CN114891004B (en) * 2017-12-23 2024-01-05 浙江九洲药业股份有限公司 Preparation method of sitagliptin intermediate compound
CN108178761A (en) * 2017-12-28 2018-06-19 安庆奇创药业有限公司 A kind of synthetic method of Xi Gelieting
CN109761988B (en) * 2019-01-17 2021-07-23 深圳市第二人民医院 Preparation method of sitagliptin serving as medicine for treating diabetes
CN110759914A (en) * 2019-02-03 2020-02-07 美华东进国际生物医药研究院有限公司 Preparation method of medicine for treating diabetes
CN112300017B (en) 2019-08-01 2023-06-09 浙江九洲药业股份有限公司 Racemization preparation method of chiral beta-amino acid and derivative thereof
CN114075201B (en) * 2020-08-20 2023-08-22 北京新康哌森医药科技有限公司 Preparation method of sitagliptin impurity
WO2024121301A1 (en) 2022-12-09 2024-06-13 Krka, D.D., Novo Mesto Process for the preparation of sitagliptin
CN116082346A (en) * 2023-04-12 2023-05-09 宙晟智维生命科学(上海)有限公司 High-fluidity sitagliptin phosphate monohydrate crystal and preparation method thereof

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Patent Citations (2)

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Publication number Priority date Publication date Assignee Title
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CN1832949A (en) * 2003-06-24 2006-09-13 麦克公司 Phosphoric acid salt of a dipeptidyl peptidase-iv inhibitor

Non-Patent Citations (1)

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Title
AHN JIN HEE ET AL.: "Synthesis, Biological Evaluation And Structural Determination Of beta- minoacyl-containing Cyclic Hydrazine Derivatives As Dipeptidyl Peptidase IV (DPP-IV) nhibitors.", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 17, 2007, pages 2622 - 2628 *

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Publication number Publication date
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