MA27765A1 - Procede de preparation de 2-cyanopyrrolidines n-substituees - Google Patents
Procede de preparation de 2-cyanopyrrolidines n-substitueesInfo
- Publication number
- MA27765A1 MA27765A1 MA28559A MA28559A MA27765A1 MA 27765 A1 MA27765 A1 MA 27765A1 MA 28559 A MA28559 A MA 28559A MA 28559 A MA28559 A MA 28559A MA 27765 A1 MA27765 A1 MA 27765A1
- Authority
- MA
- Morocco
- Prior art keywords
- compound
- reacting
- preparation
- substituted
- isolation
- Prior art date
Links
- 238000000034 method Methods 0.000 title abstract 2
- 238000002360 preparation method Methods 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 4
- ZMXDDKWLCZADIW-UHFFFAOYSA-N N,N-Dimethylformamide Chemical compound CN(C)C=O ZMXDDKWLCZADIW-UHFFFAOYSA-N 0.000 abstract 3
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 238000002955 isolation Methods 0.000 abstract 2
- VLJNHYLEOZPXFW-BYPYZUCNSA-N L-prolinamide Chemical compound NC(=O)[C@@H]1CCCN1 VLJNHYLEOZPXFW-BYPYZUCNSA-N 0.000 abstract 1
- -1 N- (N-substituted glycyl) -2-cyanopyrrolidine Chemical class 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 150000001412 amines Chemical class 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 239000012024 dehydrating agents Substances 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
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
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Diabetes (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Epidemiology (AREA)
- Pyrrole Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
La présente invention concerne un procédé de préparation de N-(glycyle N'-substitué)-2-cyanopyrrolidine comprenant au moins les étapes suivantes: (a) mise en réaction, en présence de diméthylformamide, d'un composé correspondant à la formule (V), dans laquelle X1 et X3 représentent, indépendamment l'un de l'autre, halogène, X2 représente halogène, OH, O-C(=O)-CH2X3, -O-SO2-(C1-8)alkyle ou -O-SO2-(aryle), avec du L-prolinamide ; (b) mise en réaction du composé ainsi obtenu, sans isolation, avec un agent déshydratant; et éventuellement, (c) mise en réaction, en présence d'une base, du composé ainsi obtenu, sans isolation, avec une amine appropriée; et (d) récupération du composé ainsi obtenu sous forme libre ou sous forme d'un sel d'addition d'acide.
Applications Claiming Priority (2)
| 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 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MA27765A1 true MA27765A1 (fr) | 2006-02-01 |
Family
ID=33301223
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MA28559A MA27765A1 (fr) | 2003-04-16 | 2005-10-19 | Procede de preparation de 2-cyanopyrrolidines n-substituees |
Country Status (30)
| Country | Link |
|---|---|
| US (1) | US7375238B2 (fr) |
| EP (1) | EP1620396B1 (fr) |
| JP (1) | JP4672647B2 (fr) |
| KR (1) | KR101192538B1 (fr) |
| AR (1) | AR044019A1 (fr) |
| AU (2) | AU2004230245B2 (fr) |
| BR (1) | BRPI0409471B8 (fr) |
| CA (1) | CA2520128C (fr) |
| CL (1) | CL2004000804A1 (fr) |
| CO (1) | CO5700735A2 (fr) |
| CY (1) | CY1116008T1 (fr) |
| DK (1) | DK1620396T3 (fr) |
| EC (1) | ECSP056093A (fr) |
| ES (1) | ES2531084T3 (fr) |
| HR (1) | HRP20150163T1 (fr) |
| IL (1) | IL170887A (fr) |
| IS (1) | IS2979B (fr) |
| MA (1) | MA27765A1 (fr) |
| MX (1) | MXPA05011073A (fr) |
| MY (1) | MY139476A (fr) |
| NO (1) | NO333251B1 (fr) |
| NZ (1) | NZ542899A (fr) |
| PE (2) | PE20081293A1 (fr) |
| PL (1) | PL1620396T3 (fr) |
| PT (1) | PT1620396E (fr) |
| RU (1) | RU2369598C2 (fr) |
| SG (1) | SG160212A1 (fr) |
| SI (1) | SI1620396T1 (fr) |
| TW (1) | TWI359135B (fr) |
| WO (1) | WO2004092127A1 (fr) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PE20081293A1 (es) | 2003-04-16 | 2008-11-04 | Novartis Ag | Procedimiento de preparacion de compuestos 2(s)-cianopirrolidina n-(n'-glicilo sustituida) |
| DK3366283T3 (da) | 2004-01-20 | 2021-11-22 | Novartis Ag | Direkte sammenpresningsformulering og fremgangsmåde |
| GT200600008A (es) | 2005-01-18 | 2006-08-09 | Formulacion de compresion directa y proceso | |
| EP1888562B1 (fr) | 2005-04-22 | 2014-06-18 | Alantos Pharmaceuticals Holding, Inc. | Inhibiteurs de la dipeptidyl peptidase iv |
| US20080279932A1 (en) * | 2005-08-04 | 2008-11-13 | Jean-Louis Reber | Compounds |
| 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 (fr) * | 2007-01-10 | 2008-07-17 | Medichem, S.A. | Procédé de préparation de la vildagliptine |
| 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 |
| WO2013179300A2 (fr) * | 2012-05-04 | 2013-12-05 | Megafine Pharma (P) Ltd. | Procédé de préparation de vildagliptine et de son intermédiaire |
| 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 (fr) * | 2014-03-28 | 2015-10-01 | Laurus Labs Private Limited | Procédé amélioré de préparation de vildagliptine |
| WO2021234430A1 (fr) | 2020-05-17 | 2021-11-25 | Lotus International Pte. Ltd. | Forme galénique à libération modifiée comprenant de la vildagliptine et son procédé de fabrication |
| WO2022003405A1 (fr) | 2020-07-03 | 2022-01-06 | Savoi Guilherme | Procédé monotope permettant d'obtenir un composé intermédiaire pyrrolidine-2-carbonitrile et procédé télescopique à l'échelle industrielle permettant de préparer du (2s)-1-[n-(3-hydroxyadamantan-1-yl)glycyl]-2-pyrrolidinecarbonitrile (vildagliptine) l'utilisant |
Family Cites Families (8)
| 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 |
| JP2003520849A (ja) * | 2000-01-24 | 2003-07-08 | ノボ ノルディスク アクティーゼルスカブ | 酵素ｄｐｐ−ｉｖの阻害剤であるｎ−置換２−シアノピロールおよび−ピロリン |
| 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 |
| PE20081293A1 (es) | 2003-04-16 | 2008-11-04 | Novartis Ag | Procedimiento de preparacion de compuestos 2(s)-cianopirrolidina n-(n'-glicilo sustituida) |
-
2004
- 2004-04-14 PE PE2007000421A patent/PE20081293A1/es not_active Application Discontinuation
- 2004-04-14 AR ARP040101251A patent/AR044019A1/es not_active Application Discontinuation
- 2004-04-14 PE PE2004000370A patent/PE20050021A1/es not_active Application Discontinuation
- 2004-04-15 PT PT04727557T patent/PT1620396E/pt unknown
- 2004-04-15 AU AU2004230245A patent/AU2004230245B2/en not_active Ceased
- 2004-04-15 MX MXPA05011073A patent/MXPA05011073A/es active IP Right Grant
- 2004-04-15 ES ES04727557T patent/ES2531084T3/es not_active Expired - Lifetime
- 2004-04-15 RU RU2005135331/04A patent/RU2369598C2/ru active
- 2004-04-15 SG SG200716949-3A patent/SG160212A1/en unknown
- 2004-04-15 NZ NZ542899A patent/NZ542899A/en not_active IP Right Cessation
- 2004-04-15 KR KR1020057019568A patent/KR101192538B1/ko not_active Expired - Fee Related
- 2004-04-15 WO PCT/EP2004/003980 patent/WO2004092127A1/fr not_active Ceased
- 2004-04-15 PL PL04727557T patent/PL1620396T3/pl unknown
- 2004-04-15 US US10/552,835 patent/US7375238B2/en not_active Expired - Fee Related
- 2004-04-15 DK DK04727557.3T patent/DK1620396T3/en active
- 2004-04-15 CA CA2520128A patent/CA2520128C/fr not_active Expired - Fee Related
- 2004-04-15 CL CL200400804A patent/CL2004000804A1/es unknown
- 2004-04-15 MY MYPI20041383A patent/MY139476A/en unknown
- 2004-04-15 HR HRP20150163TT patent/HRP20150163T1/hr unknown
- 2004-04-15 BR BRPI0409471A patent/BRPI0409471B8/pt not_active IP Right Cessation
- 2004-04-15 JP JP2006505132A patent/JP4672647B2/ja not_active Expired - Lifetime
- 2004-04-15 EP EP04727557.3A patent/EP1620396B1/fr not_active Expired - Lifetime
- 2004-04-15 TW TW093110566A patent/TWI359135B/zh not_active IP Right Cessation
- 2004-04-15 SI SI200432220T patent/SI1620396T1/sl unknown
-
2005
- 2005-09-15 IL IL170887A patent/IL170887A/en active IP Right Grant
- 2005-10-12 EC EC2005006093A patent/ECSP056093A/es unknown
- 2005-10-19 MA MA28559A patent/MA27765A1/fr unknown
- 2005-11-03 CO CO05112189A patent/CO5700735A2/es not_active Application Discontinuation
- 2005-11-07 NO NO20055226A patent/NO333251B1/no not_active IP Right Cessation
- 2005-11-10 IS IS8122A patent/IS2979B/is unknown
-
2008
- 2008-05-22 AU AU2008202278A patent/AU2008202278A1/en not_active Abandoned
-
2015
- 2015-02-18 CY CY20151100168T patent/CY1116008T1/el unknown
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