CN102574856B - 西他列汀的合成 - Google Patents

西他列汀的合成 Download PDF

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Publication number
CN102574856B
CN102574856B CN201080031317.1A CN201080031317A CN102574856B CN 102574856 B CN102574856 B CN 102574856B CN 201080031317 A CN201080031317 A CN 201080031317A CN 102574856 B CN102574856 B CN 102574856B
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China
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acid
amino
sitagliptin
ester
enantiomerically enriched
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Expired - Fee Related
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English (en)
Chinese (zh)
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CN102574856A (zh
Inventor
维纳亚克·戈文德·戈雷
马赫什库马·加达卡尔
普里扬卡·博斯勒
苏雷什·辛德
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Generics UK Ltd
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Generics UK Ltd
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    • 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
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A61P3/06—Antihyperlipidemics
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/02—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C229/34—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton containing six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Diabetes (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201080031317.1A 2009-05-11 2010-05-10 西他列汀的合成 Expired - Fee Related CN102574856B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
IN722/KOL/2009 2009-05-11
IN722KO2009 2009-05-11
PCT/GB2010/050760 WO2010131025A1 (en) 2009-05-11 2010-05-10 Sitagliptin synthesis

Publications (2)

Publication Number Publication Date
CN102574856A CN102574856A (zh) 2012-07-11
CN102574856B true CN102574856B (zh) 2016-09-21

Family

ID=42312921

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201080031317.1A Expired - Fee Related CN102574856B (zh) 2009-05-11 2010-05-10 西他列汀的合成

Country Status (8)

Country Link
US (1) US8846916B2 (https=)
EP (1) EP2430025A1 (https=)
JP (2) JP6199556B2 (https=)
CN (1) CN102574856B (https=)
AU (1) AU2010247193B2 (https=)
CA (1) CA2759077C (https=)
NZ (1) NZ596713A (https=)
WO (1) WO2010131025A1 (https=)

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EP2508506A1 (en) 2011-04-08 2012-10-10 LEK Pharmaceuticals d.d. Preparation of sitagliptin intermediates
CN102757431B (zh) * 2011-04-24 2016-03-30 浙江华海药业股份有限公司 一种合成西他列汀的新方法
EP2726484A1 (en) 2011-06-29 2014-05-07 Ranbaxy Laboratories Limited Solid dispersions of sitagliptin and processes for their preparation
WO2013001457A1 (en) 2011-06-30 2013-01-03 Ranbaxy Laboratories Limited Novel salts of sitagliptin
EA024688B1 (ru) * 2011-07-27 2016-10-31 ФАРМА ДжРС, Д.О.О. Способ получения ситаглиптина и его фармацевтически приемлемых солей
CN102603749B (zh) * 2011-10-27 2017-02-08 浙江华海药业股份有限公司 一种西他列汀中间体的合成方法
EP2788352A1 (en) 2011-12-08 2014-10-15 Ranbaxy Laboratories Limited Amorphous form of sitagliptin salts
CN102531937A (zh) * 2011-12-31 2012-07-04 浙江工业大学 一种化学拆分法制备(r)-3-氨基-4-(2,4,5-三氟苯基)丁酸甲酯的方法
WO2013114173A1 (en) * 2012-01-30 2013-08-08 Smilax Laboratories Limited A novel process for the preparation of sitagliptin
CN102702205B (zh) * 2012-05-16 2014-01-15 苏州新凯生物医药技术有限公司 西他列汀的制备方法
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
KR102157917B1 (ko) * 2012-12-21 2020-09-21 레크 파마슈티칼스 디.디. 키랄 γ-아릴-β-아미노부티르산 유도체의 제조를 위한 효소 경로
IN2013MU00916A (https=) * 2013-03-20 2015-06-26 Cadila Healthcare Ltd
CN103497145B (zh) * 2013-10-10 2016-01-27 南昌大学 一种光学纯多奈哌齐的制备工艺
IN2014MU00212A (https=) * 2014-01-21 2015-08-28 Cadila Healthcare Ltd
CN104557944B (zh) * 2014-12-31 2017-05-31 北京瑞都医药科技有限公司 一种降糖药物及其制备方法
CN105331651B (zh) * 2015-11-25 2018-11-13 尚科生物医药（上海）有限公司 西他列汀及其中间体的酶-化学制备方法
CN105294479B (zh) * 2015-12-05 2017-09-22 新发药业有限公司 一种3r‑氨基取代丁酰胺衍生物的制备方法
JP6049923B1 (ja) 2016-02-18 2016-12-21 三菱日立パワーシステムズ株式会社 部品情報検索装置、部品情報検索方法、およびプログラム
CN107129501B (zh) * 2017-05-19 2019-05-21 贵州大学 2型糖尿病药物西他列汀制备新方法
CN107669683B (zh) * 2017-09-30 2020-07-03 杭州华东医药集团新药研究院有限公司 含有西格列汀与二甲双胍的药物组合物
CN108586346B (zh) 2018-05-10 2019-10-01 北京富盛嘉华医药科技有限公司 一种生物催化合成西他列汀及其中间体的方法
CN110759914A (zh) * 2019-02-03 2020-02-07 美华东进国际生物医药研究院有限公司 一种治疗糖尿病的药物的制备方法
CN112300017B (zh) * 2019-08-01 2023-06-09 浙江九洲药业股份有限公司 一种手性β-氨基酸及其衍生物的消旋制备方法
CN112341332B (zh) * 2020-11-11 2023-04-28 浙江昌明药业有限公司 一种西他列汀关键中间体降解废弃物的回收利用方法
CN114644568B (zh) * 2020-12-21 2024-07-19 浙江医药股份有限公司新昌制药厂 西格列汀中间体的纯化方法
CN113045448A (zh) * 2021-03-09 2021-06-29 台州市生物医化产业研究院有限公司 一种乙酰麦氏酸衍生物降解废弃物的回收利用方法
CN115583935A (zh) * 2022-11-03 2023-01-10 浙江工业大学 一种4-(2,4,5-三氟苯基)-3-氧丁酸酯的制备方法
EP4630568A1 (en) 2022-12-09 2025-10-15 KRKA, D.D., Novo Mesto Process for the preparation of sitagliptin
CN115960007B (zh) * 2022-12-13 2025-02-07 浙江大学 一种利用含氮甲酰基催化剂的西格列汀中间体的制备方法
CN115819258B (zh) * 2022-12-13 2024-10-18 浙江大学 一种利用含膦氧双键催化剂的西格列汀中间体的制备方法
CN117069604A (zh) * 2023-08-22 2023-11-17 河北龙海药业有限公司 一种磷酸西格列汀杂质fp-e的制备方法及其检测方法

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WO2003004498A1 (en) * 2001-07-06 2003-01-16 Merck & Co., Inc. Beta-amino tetrahydroimidazo (1, 2-a) pyrazines and tetrahydrotrioazolo (4, 3-a) pyrazines as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
WO2006065826A2 (en) * 2004-12-15 2006-06-22 Merck & Co., Inc. Process to chiral beta amino acid derivatives by asymmetric hydrogenation
WO2009064476A1 (en) * 2007-11-13 2009-05-22 Teva Pharmaceutical Industries Ltd. Preparation of sitagliptin intermediate
WO2009084024A2 (en) * 2007-11-02 2009-07-09 Glenmark Generics Limited A process for the preparation of r-sit agliptin and its pharmaceutically acceptable salts thereof
CN101903390A (zh) * 2007-12-20 2010-12-01 雷迪博士实验室有限公司 制备西他列汀及其药学上可接受的盐的方法
CN101928289A (zh) * 2009-06-19 2010-12-29 北京海步国际医药科技发展有限公司 制备二肽基肽酶-iv抑制剂的方法

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WO2004085661A2 (en) 2003-03-24 2004-10-07 Merck & Co., Inc Process to chiral beta-amino acid derivatives
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JO2625B1 (en) 2003-06-24 2011-11-01 ميرك شارب اند دوم كوربوريشن Phosphoric acid salts of dipeptidyl betidase inhibitor 4
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CN101903390A (zh) * 2007-12-20 2010-12-01 雷迪博士实验室有限公司 制备西他列汀及其药学上可接受的盐的方法
CN101928289A (zh) * 2009-06-19 2010-12-29 北京海步国际医药科技发展有限公司 制备二肽基肽酶-iv抑制剂的方法

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Also Published As

Publication number Publication date
EP2430025A1 (en) 2012-03-21
NZ596713A (en) 2014-10-31
US20120108598A1 (en) 2012-05-03
US8846916B2 (en) 2014-09-30
JP2012526791A (ja) 2012-11-01
CN102574856A (zh) 2012-07-11
CA2759077A1 (en) 2010-11-18
WO2010131025A1 (en) 2010-11-18
JP2016029051A (ja) 2016-03-03
JP6199556B2 (ja) 2017-09-20
AU2010247193A1 (en) 2011-12-08
AU2010247193B2 (en) 2016-05-19
CA2759077C (en) 2016-02-16

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