AR041587A1 - Proceso para la preparacion de (s,s)-cis-2-benzhidril-3- benzilaminoquinuclidina - Google Patents
Proceso para la preparacion de (s,s)-cis-2-benzhidril-3- benzilaminoquinuclidinaInfo
- Publication number
- AR041587A1 AR041587A1 ARP030103709A ARP030103709A AR041587A1 AR 041587 A1 AR041587 A1 AR 041587A1 AR P030103709 A ARP030103709 A AR P030103709A AR P030103709 A ARP030103709 A AR P030103709A AR 041587 A1 AR041587 A1 AR 041587A1
- Authority
- AR
- Argentina
- Prior art keywords
- acid
- organic
- chiral
- isomer
- cis
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
- C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Physical Education & Sports Medicine (AREA)
- Neurology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pyrrole Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Un proceso para preparar (S,S)-cis-2-benzhildril-3-bencilaminoquinuclidina. El proceso incluye los pasos de contactar un compuesto que contiene una mezcla de R- y S-isómeros y que tiene la fórmula (1) con una cantidad efectiva de un ácido orgánico quiral en presencia de un solvente orgánico y una cantidad efectiva de un ácido carboxílico para convertir el R-isómero en una sal ácida del S-isómero, en donde el solvente orgánico es capaz de solubilizar el compuesto que contiene la mezcla de R- y S-isómeros, mientras precipita la sal ácida y el ácido carboxílico orgánico es diferente del ácido orgánico quiral; neutralizando la sal ácida con una base para proveer un S-isómero de una cetona quiral de la fórmula (2) y haciendo reaccionar la cetona quiral con una amina orgánica en presencia de un ácido Lewis para proveer la correspondiente imina y reducir la imina. El compuesto puede ejercer una acción estimulatoria sobre el tejido.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US41905102P | 2002-10-16 | 2002-10-16 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR041587A1 true AR041587A1 (es) | 2005-05-26 |
Family
ID=32108014
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP030103709A AR041587A1 (es) | 2002-10-16 | 2003-10-10 | Proceso para la preparacion de (s,s)-cis-2-benzhidril-3- benzilaminoquinuclidina |
Country Status (22)
| Country | Link |
|---|---|
| US (2) | US6861526B2 (es) |
| EP (1) | EP1551833A4 (es) |
| JP (1) | JP2006506368A (es) |
| KR (1) | KR100739901B1 (es) |
| CN (1) | CN100418964C (es) |
| AP (1) | AP2005003288A0 (es) |
| AR (1) | AR041587A1 (es) |
| AU (1) | AU2003277353B2 (es) |
| BR (1) | BR0315335A (es) |
| CA (1) | CA2500635A1 (es) |
| EA (1) | EA008192B1 (es) |
| HK (1) | HK1078087A1 (es) |
| HR (1) | HRP20050328A2 (es) |
| IS (1) | IS7755A (es) |
| MX (1) | MXPA05004058A (es) |
| PA (1) | PA8586601A1 (es) |
| PE (1) | PE20040777A1 (es) |
| PL (1) | PL376218A1 (es) |
| TN (1) | TNSN05111A1 (es) |
| UY (1) | UY28024A1 (es) |
| WO (1) | WO2004035575A1 (es) |
| ZA (1) | ZA200502411B (es) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7407955B2 (en) | 2002-08-21 | 2008-08-05 | Boehringer Ingelheim Pharma Gmbh & Co., Kg | 8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions |
| LT1713504T (lt) * | 2004-01-30 | 2017-09-11 | Zoetis Services Llc | Antimikrobinis konservantas, skirtas multi-dozinėms kompozicijoms, panaudojant beta-ciklodekstrinus, skirtas skystoms vaisto formoms |
| PT1713801E (pt) * | 2004-02-02 | 2008-02-11 | Pfizer Prod Inc | Processo para a preparação de 1-(2s,3s)-2-benzidril-n-(5- -terc-butil-2-metoxibenzil)-quinuclidina-3-amina |
| DE102004054054A1 (de) * | 2004-11-05 | 2006-05-11 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Verfahren zur Herstellung chiraler 8-(3-Amino-piperidin-1-yl)-xanthine |
| PE20080251A1 (es) | 2006-05-04 | 2008-04-25 | Boehringer Ingelheim Int | Usos de inhibidores de dpp iv |
| MX2008014024A (es) | 2006-05-04 | 2008-11-14 | Boehringer Ingelheim Int | Formas poliformas. |
| EP1852108A1 (en) | 2006-05-04 | 2007-11-07 | Boehringer Ingelheim Pharma GmbH & Co.KG | DPP IV inhibitor formulations |
| PE20091730A1 (es) | 2008-04-03 | 2009-12-10 | Boehringer Ingelheim Int | Formulaciones que comprenden un inhibidor de dpp4 |
| UY32030A (es) | 2008-08-06 | 2010-03-26 | Boehringer Ingelheim Int | "tratamiento para diabetes en pacientes inapropiados para terapia con metformina" |
| BRPI0916997A2 (pt) | 2008-08-06 | 2020-12-15 | Boehringer Ingelheim International Gmbh | Inibidor de dpp-4 e seu uso |
| US20200155558A1 (en) | 2018-11-20 | 2020-05-21 | Boehringer Ingelheim International Gmbh | Treatment for diabetes in patients with insufficient glycemic control despite therapy with an oral antidiabetic drug |
| CN107011345A (zh) | 2008-12-23 | 2017-08-04 | 勃林格殷格翰国际有限公司 | 有机化合物的盐形式 |
| AR074990A1 (es) | 2009-01-07 | 2011-03-02 | Boehringer Ingelheim Int | Tratamiento de diabetes en pacientes con un control glucemico inadecuado a pesar de la terapia con metformina |
| EP3646859A1 (en) | 2009-11-27 | 2020-05-06 | Boehringer Ingelheim International GmbH | Treatment of genotyped diabetic patients with dpp-iv inhibitors such as linagliptin |
| AU2011249722B2 (en) | 2010-05-05 | 2015-09-17 | Boehringer Ingelheim International Gmbh | Combination therapy |
| BR112012032579B1 (pt) | 2010-06-24 | 2021-05-11 | Boehringer Ingelheim International Gmbh | uso de linagliptina e composição farmacêutica compreendendo linagliptina e insulina basal de longa duração |
| US9034883B2 (en) | 2010-11-15 | 2015-05-19 | Boehringer Ingelheim International Gmbh | Vasoprotective and cardioprotective antidiabetic therapy |
| HUE043540T2 (hu) | 2011-07-15 | 2019-08-28 | Boehringer Ingelheim Int | Szubsztituált dimer kinazolin-származék, elõállítása, valamint alkalmazása 1-es és 2-es típusú cukorbetegség kezelésére szolgáló gyógyászati készítményekben |
| US9555001B2 (en) | 2012-03-07 | 2017-01-31 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition and uses thereof |
| EP3685839A1 (en) | 2012-05-14 | 2020-07-29 | Boehringer Ingelheim International GmbH | Linagliptin for use in the treatment of albuminuria and kidney related diseases |
| WO2013174767A1 (en) | 2012-05-24 | 2013-11-28 | Boehringer Ingelheim International Gmbh | A xanthine derivative as dpp -4 inhibitor for use in modifying food intake and regulating food preference |
| ES2950384T3 (es) | 2014-02-28 | 2023-10-09 | Boehringer Ingelheim Int | Uso médico de un inhibidor de DPP-4 |
| BR112018072401A2 (pt) | 2016-06-10 | 2019-02-19 | Boehringer Ingelheim International Gmbh | combinações de linagliptina e metformina |
| CN108341811A (zh) * | 2017-01-23 | 2018-07-31 | 科贝源(北京)生物医药科技有限公司 | 马罗皮坦杂质的制备方法 |
| CN108341812A (zh) * | 2017-01-23 | 2018-07-31 | 科贝源(北京)生物医药科技有限公司 | 一种含奎宁环化合物的制备方法 |
| CN106977512B (zh) * | 2017-05-04 | 2019-01-01 | 海门慧聚药业有限公司 | 制备马罗匹坦游离碱的方法 |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3560510A (en) * | 1969-03-05 | 1971-02-02 | Aldrich Chem Co Inc | 2-benzhydrylquinuclidines |
| US4680283A (en) | 1984-09-26 | 1987-07-14 | Merck & Co., Inc. | Analogs of substance P and eledoisin |
| MX18467A (es) * | 1988-11-23 | 1993-07-01 | Pfizer | Agentes terapeuticos de quinuclidinas |
| US5138060A (en) | 1991-01-03 | 1992-08-11 | Pfizer Inc. | Process and intermediates for preparing azabicyclo(2.2.2)octan-3-imines |
| HUT65771A (en) * | 1991-05-22 | 1994-07-28 | Pfizer | Process for producing substituted 3-amino-quinuclidine derivatives and pharmaceutical compositions containing them |
| UA27776C2 (uk) | 1991-05-31 | 2000-10-16 | Пфайзер Інк. | Похідні хінуклідину та їх фармацевтично прийнятні солі, що є антагоністами речовини р у ссавців, фармацевтична композиція, що має антагоністичну дію на речовину р у ссавців |
| US5721255A (en) | 1992-08-19 | 1998-02-24 | Pfizer Inc. | Substituted benzylamino nitrogen containing non-aromatic heterocycles |
| JP2656699B2 (ja) | 1992-10-21 | 1997-09-24 | ファイザー製薬株式会社 | 置換ベンジルアミノキヌクリジン |
| US5604241A (en) * | 1992-10-21 | 1997-02-18 | Pfizer Inc. | Substituted benzylaminoquinuclidines as substance P antagonists |
| JP2656700B2 (ja) | 1992-10-28 | 1997-09-24 | ファイザー製薬株式会社 | 置換キヌクリジン誘導体 |
| ES2096312T3 (es) | 1992-11-12 | 1997-03-01 | Pfizer | Derivado de quinuclidina como antagonista de la sustancia p. |
| IL109646A0 (en) | 1993-05-19 | 1994-08-26 | Pfizer | Heteroatom substituted alkyl benzylamino-quinuclidines |
| PE8798A1 (es) * | 1995-07-17 | 1998-03-02 | Pfizer | Procedimiento de separacion de los enantiomeros del 1-azabiciclo[2.2.2] octan-3-amina, 2-(difenilmetil) -n- [[2-metoxi-5-(1-metiletil) fenil] metil] |
| MX9706944A (es) | 1996-09-12 | 1998-08-30 | Pfizer | Quinuclidinas sustituidas con tetrazolilo como antagonistas de la sustancia p. |
-
2003
- 2003-10-06 US US10/679,961 patent/US6861526B2/en not_active Expired - Fee Related
- 2003-10-10 CA CA002500635A patent/CA2500635A1/en not_active Abandoned
- 2003-10-10 AR ARP030103709A patent/AR041587A1/es unknown
- 2003-10-10 AP AP2005003288A patent/AP2005003288A0/xx unknown
- 2003-10-10 EA EA200500650A patent/EA008192B1/ru not_active IP Right Cessation
- 2003-10-10 KR KR1020057006471A patent/KR100739901B1/ko not_active IP Right Cessation
- 2003-10-10 CN CNB200380101563XA patent/CN100418964C/zh not_active Expired - Fee Related
- 2003-10-10 JP JP2004544849A patent/JP2006506368A/ja active Pending
- 2003-10-10 AU AU2003277353A patent/AU2003277353B2/en not_active Ceased
- 2003-10-10 WO PCT/US2003/032275 patent/WO2004035575A1/en active IP Right Grant
- 2003-10-10 PL PL03376218A patent/PL376218A1/xx not_active Application Discontinuation
- 2003-10-10 BR BR0315335-5A patent/BR0315335A/pt not_active IP Right Cessation
- 2003-10-10 MX MXPA05004058A patent/MXPA05004058A/es active IP Right Grant
- 2003-10-10 EP EP03808986A patent/EP1551833A4/en not_active Withdrawn
- 2003-10-14 PE PE2003001050A patent/PE20040777A1/es not_active Application Discontinuation
- 2003-10-15 UY UY28024A patent/UY28024A1/es not_active Application Discontinuation
- 2003-10-16 PA PA20038586601A patent/PA8586601A1/es unknown
-
2004
- 2004-10-27 US US10/974,447 patent/US20050085641A1/en not_active Abandoned
-
2005
- 2005-03-17 IS IS7755A patent/IS7755A/is unknown
- 2005-03-23 ZA ZA200502411A patent/ZA200502411B/en unknown
- 2005-04-13 HR HR20050328A patent/HRP20050328A2/xx not_active Application Discontinuation
- 2005-04-15 TN TNP2005000111A patent/TNSN05111A1/en unknown
-
2006
- 2006-01-16 HK HK06100706.9A patent/HK1078087A1/xx not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| BR0315335A (pt) | 2005-08-16 |
| US6861526B2 (en) | 2005-03-01 |
| JP2006506368A (ja) | 2006-02-23 |
| EA200500650A1 (ru) | 2005-10-27 |
| TNSN05111A1 (en) | 2007-05-14 |
| KR20050083764A (ko) | 2005-08-26 |
| US20040116704A1 (en) | 2004-06-17 |
| EA008192B1 (ru) | 2007-04-27 |
| PL376218A1 (en) | 2005-12-27 |
| PE20040777A1 (es) | 2004-11-20 |
| MXPA05004058A (es) | 2005-06-08 |
| CN1705664A (zh) | 2005-12-07 |
| EP1551833A4 (en) | 2010-06-02 |
| CA2500635A1 (en) | 2004-04-29 |
| UY28024A1 (es) | 2004-05-31 |
| WO2004035575A1 (en) | 2004-04-29 |
| ZA200502411B (en) | 2006-05-31 |
| IS7755A (is) | 2005-03-17 |
| EP1551833A1 (en) | 2005-07-13 |
| WO2004035575A8 (en) | 2005-05-12 |
| CN100418964C (zh) | 2008-09-17 |
| AP2005003288A0 (en) | 2005-06-30 |
| AU2003277353B2 (en) | 2007-08-09 |
| PA8586601A1 (es) | 2005-02-04 |
| KR100739901B1 (ko) | 2007-07-13 |
| HK1078087A1 (en) | 2006-03-03 |
| AU2003277353A1 (en) | 2004-05-04 |
| US20050085641A1 (en) | 2005-04-21 |
| HRP20050328A2 (en) | 2005-06-30 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |