NO333251B1 - Fremgangsmate for fremstilling av N-substituerte 2-cyanopyrrolidoner - Google Patents

Fremgangsmate for fremstilling av N-substituerte 2-cyanopyrrolidoner

Info

Publication number
NO333251B1
NO333251B1 NO20055226A NO20055226A NO333251B1 NO 333251 B1 NO333251 B1 NO 333251B1 NO 20055226 A NO20055226 A NO 20055226A NO 20055226 A NO20055226 A NO 20055226A NO 333251 B1 NO333251 B1 NO 333251B1
Authority
NO
Norway
Prior art keywords
reaction
preparation
resulting compound
substituted
cyanopyrrolidones
Prior art date
Application number
NO20055226A
Other languages
English (en)
Other versions
NO20055226L (no
Inventor
Gottfried Sedelmeier
Frank Schafer
Original Assignee
Novartis Ag
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=33301223&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=NO333251(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority claimed from GB0308854A external-priority patent/GB0308854D0/en
Priority claimed from GB0311836A external-priority patent/GB0311836D0/en
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of NO20055226L publication Critical patent/NO20055226L/no
Publication of NO333251B1 publication Critical patent/NO333251B1/no

Links

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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/401—Proline; Derivatives thereof, e.g. captopril
    • 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
    • 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

Abstract

Det er beskrevet en fremgangsmåte for fremstilling av et N-(N'-substituert glycyl)-2- cyanopyrrolidin som omfatter minst (a) omsetning i nærvær av dimetylformamid, av en forbindelse av formel (V) hvor, uavhengig av hverandre, X, og Xa er halogen, X2 er halogen, OH, O-C(=O)-CH2X3, -O-SO2-(1-8)alkyl eller-O-SO2- (aryl), med L-prolinamid, etterfulgt av b) omsetning av den resulterende forbindelsen uten isolering med et dehydratiseringsmiddel, eventuelt etterfulgt av c) omsetning, i nærvær av en base, av den resulterende forbindelsen uten isolering med et egnet amin og d) utvinning av den resulterende forbindelsen i fri form eller i syreaddisjonssaltform.
NO20055226A 2003-04-16 2005-11-07 Fremgangsmate for fremstilling av N-substituerte 2-cyanopyrrolidoner NO333251B1 (no)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB0308854A GB0308854D0 (en) 2003-04-16 2003-04-16 Organic compounds
GB0311836A GB0311836D0 (en) 2003-05-22 2003-05-22 Process for the manufacture of organic compounds
PCT/EP2004/003980 WO2004092127A1 (en) 2003-04-16 2004-04-15 Process for the preparation of n-substituted 2-cyanopyrrolidines

Publications (2)

Publication Number Publication Date
NO20055226L NO20055226L (no) 2005-11-07
NO333251B1 true NO333251B1 (no) 2013-04-22

Family

ID=33301223

Family Applications (1)

Application Number Title Priority Date Filing Date
NO20055226A NO333251B1 (no) 2003-04-16 2005-11-07 Fremgangsmate for fremstilling av N-substituerte 2-cyanopyrrolidoner

Country Status (31)

Country Link
US (1) US7375238B2 (no)
EP (1) EP1620396B1 (no)
JP (1) JP4672647B2 (no)
KR (1) KR101192538B1 (no)
AR (1) AR044019A1 (no)
AU (2) AU2004230245B2 (no)
BR (1) BRPI0409471B8 (no)
CA (1) CA2520128C (no)
CL (1) CL2004000804A1 (no)
CO (1) CO5700735A2 (no)
CY (1) CY1116008T1 (no)
DK (1) DK1620396T3 (no)
EC (1) ECSP056093A (no)
ES (1) ES2531084T3 (no)
HK (1) HK1087695A1 (no)
HR (1) HRP20150163T1 (no)
IL (1) IL170887A (no)
IS (1) IS2979B (no)
MA (1) MA27765A1 (no)
MX (1) MXPA05011073A (no)
MY (1) MY139476A (no)
NO (1) NO333251B1 (no)
NZ (1) NZ542899A (no)
PE (2) PE20081293A1 (no)
PL (1) PL1620396T3 (no)
PT (1) PT1620396E (no)
RU (1) RU2369598C2 (no)
SG (1) SG160212A1 (no)
SI (1) SI1620396T1 (no)
TW (1) TWI359135B (no)
WO (1) WO2004092127A1 (no)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR044019A1 (es) 2003-04-16 2005-08-24 Novartis Ag Proceso para la preparacion de 2-cianopirrolidinas n-sustituidas
PT1715893E (pt) 2004-01-20 2009-10-20 Novartis Pharma Ag Formulação para compressão directa e processos
GT200600008A (es) 2005-01-18 2006-08-09 Formulacion de compresion directa y proceso
BRPI0614610A2 (pt) * 2005-08-04 2011-04-05 Novartis Ag compostos
WO2008066083A1 (fr) * 2006-11-29 2008-06-05 Mitsubishi Tanabe Pharma Corporation Procédé de production d'un dérivé de n-(n'-glycyle substitué)-2-cyanopyrrolidine
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
EA034049B1 (ru) * 2009-07-31 2019-12-23 КРКА, д.д., НОВО МЕСТО Гранулят, включающий вилдаглиптин, способ его получения и фармацевтическая композиция
HUP0900638A2 (en) * 2009-10-07 2011-05-30 Egyt Gyogyszervegyeszeti Gyar Adducts of inorganic salts basea on vildaelitpin applicable for preparation of pharmaceutical compositions
IT1400714B1 (it) 2010-07-06 2013-06-28 Chemelectiva S R L Processo ed intermedi per la preparazione di un principio attivo.
HU231050B1 (hu) 2010-08-19 2020-02-28 Egis Gyógyszergyár Nyrt. Eljárás gyógyszerhatóanyag előállítására
ITMI20112224A1 (it) * 2011-12-06 2013-06-07 Chemelectiva S R L Nuovo processo ed intermedi per la sintesi di vildagliptin
IN2012MU01383A (no) * 2012-05-04 2014-02-28
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
WO2015145467A1 (en) * 2014-03-28 2015-10-01 Laurus Labs Private Limited An improved process for preparing vildagliptin
WO2021234430A1 (en) 2020-05-17 2021-11-25 Lotus International Pte. Ltd. Modified release dosage form comprising vildagliptin and process for manufacturing the same
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 (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5510369A (en) * 1994-07-22 1996-04-23 Merck & Co., Inc. Pyrrolidine thrombin inhibitors
TW492957B (en) * 1996-11-07 2002-07-01 Novartis Ag N-substituted 2-cyanopyrrolidnes
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
US6380398B2 (en) * 2000-01-04 2002-04-30 Novo Nordisk A/S Therapeutically active and selective heterocyclic compounds that are inhibitors of the enzyme DPP-IV
EP1254113A1 (en) * 2000-01-24 2002-11-06 Novo Nordisk A/S N-substituted 2-cyanopyroles and -pyrrolines which are inhibitors of the enzyme dpp-iv
TW583185B (en) * 2000-06-13 2004-04-11 Novartis Ag N-(substituted glycyl)-2-cyanopyrrolidines and pharmaceutical composition for inhibiting dipeptidyl peptidase-IV (DPP-IV) or for the prevention or treatment of diseases or conditions associated with elevated levels of DPP-IV comprising the same
JP2002265439A (ja) * 2001-03-08 2002-09-18 Mitsubishi Pharma Corp シアノピロリジン誘導体およびその医薬用途
AR044019A1 (es) 2003-04-16 2005-08-24 Novartis Ag Proceso para la preparacion de 2-cianopirrolidinas n-sustituidas

Also Published As

Publication number Publication date
KR101192538B1 (ko) 2012-10-17
CA2520128A1 (en) 2004-10-28
IL170887A (en) 2013-06-27
IS8122A (is) 2005-11-10
PL1620396T3 (pl) 2015-05-29
KR20060003878A (ko) 2006-01-11
ES2531084T3 (es) 2015-03-10
TW200510299A (en) 2005-03-16
BRPI0409471B1 (pt) 2015-11-03
TWI359135B (en) 2012-03-01
CA2520128C (en) 2012-02-07
EP1620396B1 (en) 2014-12-03
MY139476A (en) 2009-10-30
RU2369598C2 (ru) 2009-10-10
NO20055226L (no) 2005-11-07
JP4672647B2 (ja) 2011-04-20
CO5700735A2 (es) 2006-11-30
WO2004092127A1 (en) 2004-10-28
AU2004230245A1 (en) 2004-10-28
RU2005135331A (ru) 2006-06-27
US20060199854A1 (en) 2006-09-07
JP2006523645A (ja) 2006-10-19
NZ542899A (en) 2009-02-28
AU2008202278A1 (en) 2008-11-20
US7375238B2 (en) 2008-05-20
MA27765A1 (fr) 2006-02-01
EP1620396A1 (en) 2006-02-01
PE20050021A1 (es) 2005-03-15
HK1087695A1 (en) 2006-10-20
CY1116008T1 (el) 2017-01-25
HRP20150163T1 (en) 2015-03-27
ECSP056093A (es) 2006-03-01
AU2004230245B2 (en) 2008-02-21
IS2979B (is) 2017-09-15
BRPI0409471A (pt) 2006-05-02
MXPA05011073A (es) 2005-12-12
SG160212A1 (en) 2010-04-29
AR044019A1 (es) 2005-08-24
BRPI0409471B8 (pt) 2021-05-25
PE20081293A1 (es) 2008-11-04
PT1620396E (pt) 2015-03-05
CL2004000804A1 (es) 2005-02-11
SI1620396T1 (sl) 2015-03-31
DK1620396T3 (en) 2015-02-23

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