PE20050021A1 - Procedimiento para la preparacion de 2-cianopirrolidina n-sustituida - Google Patents
Procedimiento para la preparacion de 2-cianopirrolidina n-sustituidaInfo
- Publication number
- PE20050021A1 PE20050021A1 PE2004000370A PE2004000370A PE20050021A1 PE 20050021 A1 PE20050021 A1 PE 20050021A1 PE 2004000370 A PE2004000370 A PE 2004000370A PE 2004000370 A PE2004000370 A PE 2004000370A PE 20050021 A1 PE20050021 A1 PE 20050021A1
- Authority
- PE
- Peru
- Prior art keywords
- halogen
- reacting
- procedure
- substituted
- resulting compound
- Prior art date
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
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)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
SE REFIERE A UN PROCEDIMIENTO PARA LA PREPARACION DE 2-CIANOPIRROLIDINA N-(N´-GLICILO SUSTITUIDA), DE FORMULA I, EN DONDE R ES R1R1aN(CH2)m, CICLOALQUILO C3-C12, ENTRE OTROS; R1 ES UNA PORCION PIRIDINILO O PIRIMIDINILO OPCIONALMENTE SUSTITUIDA CON ALQUILO C1-C4, ALCOXI C1-C4, HALOGENO, ENTRE OTROS; R1a ES H o ALQUILO C1-C8; m ES 2 o 3. DICHO PROCEDIMIENTO COMPRENDE POR LO MENOS: (a) HACER REACCIONAR, EN PRESENCIA DE DIMETILFORMAMIDA, UN COMPUESTO DE LA FORMULA (V), EN DONDE X1 Y X3 SON, INDEPENDIENTEMENTE ENTRE SI, HALOGENO; X2 ES HALOGENO, OH, O-C(=O)-CH2X3, ENTRE OTROS; CON L-PROLINAMIDA, SEGUIDO POR, (b) HACER REACCIONAR EL COMPUESTO RESULTANTE SIN AISLAMIENTO CON UN AGENTE DE DESHIDRATACION, OPCIONALMENTE SEGUIDO POR, (c) HACER REACCIONAR, EN PRESENCIA DE UNA BASE, EL COMPUESTO RESULTANTE SIN AISLAMIENTO CON UNA AMINA APROPIADA, Y (d) RECUPERAR EL COMPUESTO RESULTANTE EN FORMA LIBRE O EN FORMA DE SAL DE ADICION DE ACIDO. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA./1-[(3-HIDROXI-1-ADAMANTIL)AMINO]ACETIL-2-CIANO-PIRROLIDINA, LAF237
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 |
|---|---|
| PE20050021A1 true PE20050021A1 (es) | 2005-03-15 |
Family
ID=33301223
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2007000421A PE20081293A1 (es) | 2003-04-16 | 2004-04-14 | Procedimiento de preparacion de compuestos 2(s)-cianopirrolidina n-(n'-glicilo sustituida) |
| PE2004000370A PE20050021A1 (es) | 2003-04-16 | 2004-04-14 | Procedimiento para la preparacion de 2-cianopirrolidina n-sustituida |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2007000421A PE20081293A1 (es) | 2003-04-16 | 2004-04-14 | Procedimiento de preparacion de compuestos 2(s)-cianopirrolidina n-(n'-glicilo sustituida) |
Country Status (31)
| Country | Link |
|---|---|
| US (1) | US7375238B2 (es) |
| EP (1) | EP1620396B1 (es) |
| JP (1) | JP4672647B2 (es) |
| KR (1) | KR101192538B1 (es) |
| AR (1) | AR044019A1 (es) |
| AU (2) | AU2004230245B2 (es) |
| BR (1) | BRPI0409471B8 (es) |
| CA (1) | CA2520128C (es) |
| CL (1) | CL2004000804A1 (es) |
| CO (1) | CO5700735A2 (es) |
| CY (1) | CY1116008T1 (es) |
| DK (1) | DK1620396T3 (es) |
| EC (1) | ECSP056093A (es) |
| ES (1) | ES2531084T3 (es) |
| HK (1) | HK1087695A1 (es) |
| HR (1) | HRP20150163T1 (es) |
| IL (1) | IL170887A (es) |
| IS (1) | IS2979B (es) |
| MA (1) | MA27765A1 (es) |
| MX (1) | MXPA05011073A (es) |
| MY (1) | MY139476A (es) |
| NO (1) | NO333251B1 (es) |
| NZ (1) | NZ542899A (es) |
| PE (2) | PE20081293A1 (es) |
| PL (1) | PL1620396T3 (es) |
| PT (1) | PT1620396E (es) |
| RU (1) | RU2369598C2 (es) |
| SG (1) | SG160212A1 (es) |
| SI (1) | SI1620396T1 (es) |
| TW (1) | TWI359135B (es) |
| WO (1) | WO2004092127A1 (es) |
Families Citing this family (17)
| 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) |
| PL3738585T3 (pl) | 2004-01-20 | 2023-04-17 | Novartis Ag | Preparat i sposób jego bezpośredniego prasowania |
| GT200600008A (es) | 2005-01-18 | 2006-08-09 | Formulacion de compresion directa y proceso | |
| WO2007019255A2 (en) * | 2005-08-04 | 2007-02-15 | Novartis Ag | Salts of vildagliptin |
| 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 |
| US20080167479A1 (en) * | 2007-01-10 | 2008-07-10 | Medichem, S.A. | Process for preparing vildagliptin |
| CZ2008512A3 (cs) | 2008-08-26 | 2010-03-10 | Zentiva, A. S | Zpusob prípravy vysoce cistého vildagliptinu |
| WO2011012322A2 (en) | 2009-07-31 | 2011-02-03 | Krka, D.D., Novo Mesto | Synthesis and use of vildagliptin for the preparation of pharmaceutical dosage forms |
| 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 (es) | 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)
| 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 PE PE2004000370A patent/PE20050021A1/es not_active Application Discontinuation
- 2004-04-14 AR ARP040101251A patent/AR044019A1/es not_active Application Discontinuation
- 2004-04-15 TW TW093110566A patent/TWI359135B/zh not_active IP Right Cessation
- 2004-04-15 AU AU2004230245A patent/AU2004230245B2/en not_active Ceased
- 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 WO PCT/EP2004/003980 patent/WO2004092127A1/en active Application Filing
- 2004-04-15 US US10/552,835 patent/US7375238B2/en not_active Expired - Fee Related
- 2004-04-15 MX MXPA05011073A patent/MXPA05011073A/es active IP Right Grant
- 2004-04-15 PL PL04727557T patent/PL1620396T3/pl unknown
- 2004-04-15 DK DK04727557.3T patent/DK1620396T3/en active
- 2004-04-15 SG SG200716949-3A patent/SG160212A1/en unknown
- 2004-04-15 KR KR1020057019568A patent/KR101192538B1/ko active IP Right Review Request
- 2004-04-15 SI SI200432220T patent/SI1620396T1/sl unknown
- 2004-04-15 CL CL200400804A patent/CL2004000804A1/es unknown
- 2004-04-15 CA CA2520128A patent/CA2520128C/en not_active Expired - Fee Related
- 2004-04-15 JP JP2006505132A patent/JP4672647B2/ja not_active Expired - Lifetime
- 2004-04-15 BR BRPI0409471A patent/BRPI0409471B8/pt not_active IP Right Cessation
- 2004-04-15 PT PT04727557T patent/PT1620396E/pt unknown
- 2004-04-15 MY MYPI20041383A patent/MY139476A/en unknown
- 2004-04-15 NZ NZ542899A patent/NZ542899A/en not_active IP Right Cessation
- 2004-04-15 EP EP04727557.3A patent/EP1620396B1/en not_active Expired - Lifetime
-
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
-
2006
- 2006-07-11 HK HK06107769.8A patent/HK1087695A1/xx not_active IP Right Cessation
-
2008
- 2008-05-22 AU AU2008202278A patent/AU2008202278A1/en not_active Abandoned
-
2015
- 2015-02-10 HR HRP20150163TT patent/HRP20150163T1/hr unknown
- 2015-02-18 CY CY20151100168T patent/CY1116008T1/el unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant, registration | ||
| FD | Application declared void or lapsed |