ES2527191T3 - Procedimiento e intermedios para la preparación de un ingrediente activo - Google Patents

Procedimiento e intermedios para la preparación de un ingrediente activo Download PDF

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Publication number
ES2527191T3
ES2527191T3 ES11735614.7T ES11735614T ES2527191T3 ES 2527191 T3 ES2527191 T3 ES 2527191T3 ES 11735614 T ES11735614 T ES 11735614T ES 2527191 T3 ES2527191 T3 ES 2527191T3
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ES
Spain
Prior art keywords
formula
intermediates
procedure
preparation
active ingredient
Prior art date
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Active
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ES11735614.7T
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English (en)
Inventor
Marco Baratella
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
CHEMELECTIVA Srl
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CHEMELECTIVA Srl
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Filing date
Publication date
Application filed by CHEMELECTIVA Srl filed Critical CHEMELECTIVA Srl
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Publication of ES2527191T3 publication Critical patent/ES2527191T3/es
Active legal-status Critical Current
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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00—Preparation of carboxylic acid amides
    • C07C231/14—Preparation of carboxylic acid amides by formation of carboxamide groups together with reactions not involving the carboxamide groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00—Systems containing at least three condensed rings
    • C07C2603/56—Ring systems containing bridged rings
    • C07C2603/58—Ring systems containing bridged rings containing three rings
    • C07C2603/70—Ring systems containing bridged rings containing three rings containing only six-membered rings
    • C07C2603/74—Adamantanes

Landscapes

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

Abstract

Un procedimiento para la síntesis de vildagliptina que comprende las siguientes etapas: a) la reacción de 1-amino-3-adamantanol (III) con ácido glioxílico para dar el intermedio de fórmula**Fórmula** b) la reacción del intermedio (VI) con L-prolinamida para dar el intermedio de fórmula**Fórmula** c) la deshidratación del intermedio (VII) para dar el derivado de nitrilo correspondiente de fórmula**Fórmula** d) la desformilación del intermedio (VIII) para dar vildagliptina (I).

Description

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Claims (1)

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ES11735614.7T 2010-07-06 2011-07-04 Procedimiento e intermedios para la preparación de un ingrediente activo Active ES2527191T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
ITMI20101239 2010-07-06
ITMI2010A001239A IT1400714B1 (it) 2010-07-06 2010-07-06 Processo ed intermedi per la preparazione di un principio attivo.
PCT/EP2011/061178 WO2012004210A1 (en) 2010-07-06 2011-07-04 Process and intermediates for preparation of an active ingredient

Publications (1)

Publication Number Publication Date
ES2527191T3 true ES2527191T3 (es) 2015-01-21

Family

ID=43501421

Family Applications (1)

Application Number Title Priority Date Filing Date
ES11735614.7T Active ES2527191T3 (es) 2010-07-06 2011-07-04 Procedimiento e intermedios para la preparación de un ingrediente activo

Country Status (4)

Country Link
EP (1) EP2590943B1 (es)
ES (1) ES2527191T3 (es)
IT (1) IT1400714B1 (es)
WO (1) WO2012004210A1 (es)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102617434B (zh) * 2012-03-29 2014-07-23 中国科学院上海有机化学研究所 一锅法制备维达列汀
CN103922986B (zh) * 2013-01-16 2017-02-15 上海彩迩文生化科技有限公司 维大列汀及其类似物、中间体及其制备方法和应用
JP2017507934A (ja) * 2014-02-28 2017-03-23 ヒカル リミテッド ビルダグリプチンのための新規な実用的プロセス
CN105884669B (zh) * 2014-09-15 2020-05-15 深圳翰宇药业股份有限公司 制备取代的(s)-吡咯烷-2-甲腈及维格列汀的方法
CN105712919B (zh) * 2014-12-04 2018-12-21 南京优科生物医药研究有限公司 酰胺缩合剂在维格列汀合成方法中的应用
CN105712920B (zh) * 2014-12-04 2018-12-21 南京优科生物医药研究有限公司 一种维格列汀的制备方法
CN106432026A (zh) * 2016-09-12 2017-02-22 重庆医科大学 一类对糖尿病具有潜在治疗活性的化合物
WO2022003405A1 (en) 2020-07-03 2022-01-06 Savoi Guilherme One-pot process to obtain a pyrrolidine-2-carbonitrile intermediate compound and industrial scale telescopic process to prepare (2s)-1-[n-(3-hydroxyadamantan-1-yl)glycyl]-2-pyrrolidinecarbonitrile (vildagliptin) using same

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CO5150173A1 (es) 1998-12-10 2002-04-29 Novartis Ag Compuestos n-(glicilo sustituido)-2-cianopirrolidinas inhibidores de peptidasa de dipeptidilo-iv (dpp-iv) los cuales son efectivos en el tratamiento de condiciones mediadas por la inhibicion de dpp-iv
PE20050021A1 (es) 2003-04-16 2005-03-15 Novartis Ag Procedimiento para la preparacion de 2-cianopirrolidina n-sustituida
WO2008084383A2 (en) * 2007-01-10 2008-07-17 Medichem, S.A. Process for preparing vildagliptin
CZ2008512A3 (cs) 2008-08-26 2010-03-10 Zentiva, A. S Zpusob prípravy vysoce cistého vildagliptinu

Also Published As

Publication number Publication date
IT1400714B1 (it) 2013-06-28
WO2012004210A1 (en) 2012-01-12
EP2590943B1 (en) 2014-10-01
ITMI20101239A1 (it) 2012-01-07
EP2590943A1 (en) 2013-05-15

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