EA201490383A1 - Способ получения ситаглиптина и его фармацевтически приемлемых солей - Google Patents

Способ получения ситаглиптина и его фармацевтически приемлемых солей

Info

Publication number
EA201490383A1
EA201490383A1 EA201490383A EA201490383A EA201490383A1 EA 201490383 A1 EA201490383 A1 EA 201490383A1 EA 201490383 A EA201490383 A EA 201490383A EA 201490383 A EA201490383 A EA 201490383A EA 201490383 A1 EA201490383 A1 EA 201490383A1
Authority
EA
Eurasian Patent Office
Prior art keywords
formula
pharmaceutically acceptable
compound
acceptable salts
sitahliptine
Prior art date
Application number
EA201490383A
Other languages
English (en)
Other versions
EA024688B1 (ru
Inventor
Сильво Зупанциц
Рок Зупет
Original Assignee
ФАРМА ДжРС, Д.О.О.
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 ФАРМА ДжРС, Д.О.О. filed Critical ФАРМА ДжРС, Д.О.О.
Publication of EA201490383A1 publication Critical patent/EA201490383A1/ru
Publication of EA024688B1 publication Critical patent/EA024688B1/ru

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
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

В настоящем изобретении приведено описание способа получения ситаглиптина или его фармацевтически приемлемых солей формулы (1), включающего стадии: а) конденсации соединения формулы (2), в котором R представляет собой аминозащитную группу с соединением формулы (3), которое может быть использовано в форме свободного основания или в форме соли в присутствии связывающего вещества и основного растворителя, который представляет собой N-метилимидазол, с получением соединения формулы (4), и b) удаление защитной группы у соединения формулы (4), с получением основания ситаглиптина, которое может быть дополнительно переведено в его фармацевтически приемлемую соль. Указанный способ высокорентабелен, экологически безопасен, недорог и легко масштабируем до промышленного уровня.
EA201490383A 2011-07-27 2012-07-27 Способ получения ситаглиптина и его фармацевтически приемлемых солей EA024688B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
SI201100277 2011-07-27
PCT/EP2012/003214 WO2013013833A1 (en) 2011-07-27 2012-07-27 Process for the preparation of sitagliptin and its pharmaceutically acceptable salts

Publications (2)

Publication Number Publication Date
EA201490383A1 true EA201490383A1 (ru) 2014-06-30
EA024688B1 EA024688B1 (ru) 2016-10-31

Family

ID=46583953

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201490383A EA024688B1 (ru) 2011-07-27 2012-07-27 Способ получения ситаглиптина и его фармацевтически приемлемых солей

Country Status (4)

Country Link
EP (1) EP2736909B1 (ru)
EA (1) EA024688B1 (ru)
SI (1) SI2736909T1 (ru)
WO (1) WO2013013833A1 (ru)

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CN106124667B (zh) * 2016-08-29 2018-07-31 上海应用技术学院 一种分离测定西格列汀有关物质的方法
CN112209931A (zh) * 2019-07-10 2021-01-12 浙江昌海制药有限公司 一种提高西格列汀收率和纯度的工艺方法
CN113149991A (zh) * 2020-12-31 2021-07-23 浙江美诺华药物化学有限公司 西他列汀游离碱及西他列汀磷酸盐一水合物的合成方法

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Also Published As

Publication number Publication date
EP2736909B1 (en) 2017-03-29
SI2736909T1 (sl) 2017-08-31
WO2013013833A1 (en) 2013-01-31
EA024688B1 (ru) 2016-10-31
EP2736909A1 (en) 2014-06-04

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