AR011126A1 - Procedimiento para preparar eprosartano y compuestos intermediarios. - Google Patents
Procedimiento para preparar eprosartano y compuestos intermediarios.Info
- Publication number
- AR011126A1 AR011126A1 ARP980100586A ARP980100586A AR011126A1 AR 011126 A1 AR011126 A1 AR 011126A1 AR P980100586 A ARP980100586 A AR P980100586A AR P980100586 A ARP980100586 A AR P980100586A AR 011126 A1 AR011126 A1 AR 011126A1
- Authority
- AR
- Argentina
- Prior art keywords
- compound
- formula
- nitrogen
- 4alkyl
- reacting
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Hospice & Palliative Care (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Steroid Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Un procedimiento para la preparacion de eprosartano, un compuesto de formula (I): o una de sus sales farmacéuticamente aceptables que comprende lasetapas de: (i) someter a tratamiento un compuesto de formula (II): con una base, seguidode reaccion con un reactivo regioselectivo protector de nitrogeno(ii) hacer reaccionar el compuesto de formula (III); en la que R1 es un grupo protector de nitrogeno que consiste en, o bien (1) un puente de etileno queconecta el nitrogeno a ungrupo atractor del electrones, tal como un éster (COOR, donde R=alquilo C1-4), ácido, carbonilo, nitrilo, sulfona osulfoxido, o (2) un puente de metileno que conecta el nitrogeno a un pivalato, 2-(trimetilsilil)etoxi, metoxi, terc-butoxi, obenciloxi , con un compuesto deformula (IV); en la que R es alquilo C1-4 en presencia, de un catalizador; y (iii) hacer reaccionar el compuesto de formula (V); en la que R y R1 sedefinen como antes con un comupuesto de formula (VI); en la que R esalquilo C1 -4 y X es halogeno u OR+, en que R+ es CH3SO2- o p-CH3C6H4SO2-, atemperaturas elevadas; y, después de esto, hidrolizar los grupos éster R y R y separar el grupo protector de N-3 y opcionalmente formar una salfarmacéuticamenteaceptable. Este comp uesto es antagonista del receptor de la angiotensina II, util en el tratamiento de hipertension, insuficienciacardíaca congestiva e insuficiencia renal. Además se describe un procedimiento alternativo y compuestosintermediarios.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US3819697P | 1997-02-14 | 1997-02-14 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR011126A1 true AR011126A1 (es) | 2000-08-02 |
Family
ID=21898590
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP980100586A AR011126A1 (es) | 1997-02-14 | 1998-02-10 | Procedimiento para preparar eprosartano y compuestos intermediarios. |
Country Status (41)
| Country | Link |
|---|---|
| US (2) | US6294675B1 (es) |
| EP (1) | EP0973769B1 (es) |
| JP (1) | JP4227671B2 (es) |
| KR (1) | KR100551667B1 (es) |
| CN (1) | CN1093128C (es) |
| AP (1) | AP1202A (es) |
| AR (1) | AR011126A1 (es) |
| AT (1) | ATE274511T1 (es) |
| AU (1) | AU730162B2 (es) |
| BG (1) | BG63970B1 (es) |
| BR (1) | BRPI9808642B8 (es) |
| CA (1) | CA2281471C (es) |
| CO (1) | CO4950549A1 (es) |
| CY (1) | CY2551B1 (es) |
| CZ (1) | CZ296543B6 (es) |
| DE (1) | DE69825880T2 (es) |
| DK (1) | DK0973769T3 (es) |
| DZ (1) | DZ2418A1 (es) |
| EA (1) | EA001761B1 (es) |
| EG (1) | EG23780A (es) |
| ES (1) | ES2224358T3 (es) |
| HK (1) | HK1026206A1 (es) |
| HU (1) | HU228098B1 (es) |
| ID (1) | ID23155A (es) |
| IL (4) | IL131310A (es) |
| IN (1) | IN188000B (es) |
| MA (1) | MA24472A1 (es) |
| MY (1) | MY120024A (es) |
| NO (1) | NO317761B1 (es) |
| NZ (1) | NZ337182A (es) |
| OA (1) | OA11086A (es) |
| PE (1) | PE59799A1 (es) |
| PL (1) | PL192837B1 (es) |
| PT (1) | PT973769E (es) |
| SA (1) | SA98190146B1 (es) |
| SI (1) | SI0973769T1 (es) |
| SK (1) | SK285125B6 (es) |
| TR (1) | TR199901935T2 (es) |
| UA (1) | UA57060C2 (es) |
| WO (1) | WO1998035962A1 (es) |
| ZA (1) | ZA981208B (es) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR011126A1 (es) * | 1997-02-14 | 2000-08-02 | Smithkline Beecham Corp | Procedimiento para preparar eprosartano y compuestos intermediarios. |
| US6630498B2 (en) * | 1997-08-06 | 2003-10-07 | Smithkline Beecham Corporation | Eprosartan arginyl charge-neutralization-complex and a process for its preparation and formulation |
| WO2000004862A2 (en) * | 1998-07-20 | 2000-02-03 | Smithkline Beecham Corporation | Bioenhanced formulations comprising eprosartan in oral solid dosage form |
| US20060099230A1 (en) * | 2004-11-10 | 2006-05-11 | Chin-Chih Chiang | Novel formulations of eprosartan with enhanced bioavailability |
| WO2008078330A1 (en) * | 2006-12-27 | 2008-07-03 | Hetero Drugs Limited | Improved process for eprosartan |
| CA2703231A1 (en) * | 2007-10-22 | 2009-04-30 | Orchid Research Laboratories Limited | Histone deacetylase inhibitors |
| CN101215284B (zh) * | 2007-12-31 | 2010-10-13 | 浙江华海药业股份有限公司 | 一种改进的依普罗沙坦的制备方法 |
| WO2011004384A2 (en) | 2009-06-05 | 2011-01-13 | Glochem Industries Limited | Process for the preparation of eprosartan |
| CN102584709B (zh) * | 2011-12-19 | 2016-08-17 | 浙江华海药业股份有限公司 | 一种改进的依普罗沙坦中间体芳基咪唑醛的制备工艺 |
| CN103288742A (zh) * | 2013-06-04 | 2013-09-11 | 四川百利药业有限责任公司 | 一种高纯度英加韦林原料的制备方法 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5418250A (en) * | 1989-06-14 | 1995-05-23 | Smithkline Beecham Corporation | Imidazolyl-alkenoic acids useful as angiotensin II receptor antagonists |
| US5185351A (en) * | 1989-06-14 | 1993-02-09 | Smithkline Beecham Corporation | Imidazolyl-alkenoic acids useful as angiotensin II receptor antagonists |
| ES2142789T3 (es) * | 1989-06-14 | 2000-05-01 | Smithkline Beecham Corp | Acidos imidazolil-alquenoicos. |
| NZ239161A (en) * | 1990-07-31 | 1994-01-26 | Smithkline Beecham Corp | Substituted [1h-imidazol-5-yl] alkanoic acid derivatives; medicaments, |
| WO1992010189A1 (en) | 1990-12-14 | 1992-06-25 | Smithkline Beecham Corporation | Imidazolyl-alkenoic acids |
| AR011126A1 (es) * | 1997-02-14 | 2000-08-02 | Smithkline Beecham Corp | Procedimiento para preparar eprosartano y compuestos intermediarios. |
-
1998
- 1998-02-10 AR ARP980100586A patent/AR011126A1/es active IP Right Grant
- 1998-02-11 DZ DZ980028A patent/DZ2418A1/xx active
- 1998-02-11 MY MYPI98000545A patent/MY120024A/en unknown
- 1998-02-11 EG EG15498A patent/EG23780A/xx active
- 1998-02-12 MA MA24963A patent/MA24472A1/fr unknown
- 1998-02-12 PE PE1998000102A patent/PE59799A1/es not_active IP Right Cessation
- 1998-02-12 IN IN361DE1998 patent/IN188000B/en unknown
- 1998-02-13 IL IL13131098A patent/IL131310A/xx not_active IP Right Cessation
- 1998-02-13 IL IL14378598A patent/IL143785A/en not_active IP Right Cessation
- 1998-02-13 IL IL14378498A patent/IL143784A/xx not_active IP Right Cessation
- 1998-02-13 AU AU62732/98A patent/AU730162B2/en not_active Expired
- 1998-02-13 DE DE69825880T patent/DE69825880T2/de not_active Expired - Lifetime
- 1998-02-13 CO CO98007696A patent/CO4950549A1/es unknown
- 1998-02-13 ES ES98904999T patent/ES2224358T3/es not_active Expired - Lifetime
- 1998-02-13 EA EA199900741A patent/EA001761B1/ru not_active IP Right Cessation
- 1998-02-13 UA UA99084525A patent/UA57060C2/uk unknown
- 1998-02-13 TR TR1999/01935T patent/TR199901935T2/xx unknown
- 1998-02-13 ID IDW990840Q patent/ID23155A/id unknown
- 1998-02-13 US US09/355,186 patent/US6294675B1/en not_active Expired - Lifetime
- 1998-02-13 HU HU0001813A patent/HU228098B1/hu unknown
- 1998-02-13 BR BRPI9808642A patent/BRPI9808642B8/pt not_active IP Right Cessation
- 1998-02-13 CA CA002281471A patent/CA2281471C/en not_active Expired - Lifetime
- 1998-02-13 PL PL335074A patent/PL192837B1/pl unknown
- 1998-02-13 SK SK1086-99A patent/SK285125B6/sk not_active IP Right Cessation
- 1998-02-13 ZA ZA981208A patent/ZA981208B/xx unknown
- 1998-02-13 SI SI9830688T patent/SI0973769T1/xx unknown
- 1998-02-13 EP EP98904999A patent/EP0973769B1/en not_active Expired - Lifetime
- 1998-02-13 AT AT98904999T patent/ATE274511T1/de active
- 1998-02-13 JP JP53584098A patent/JP4227671B2/ja not_active Expired - Lifetime
- 1998-02-13 AP APAP/P/1999/001619A patent/AP1202A/en active
- 1998-02-13 IL IL14378398A patent/IL143783A/xx not_active IP Right Cessation
- 1998-02-13 WO PCT/US1998/002411 patent/WO1998035962A1/en active IP Right Grant
- 1998-02-13 PT PT98904999T patent/PT973769E/pt unknown
- 1998-02-13 DK DK98904999T patent/DK0973769T3/da active
- 1998-02-13 KR KR1019997007274A patent/KR100551667B1/ko not_active IP Right Cessation
- 1998-02-13 NZ NZ337182A patent/NZ337182A/en not_active IP Right Cessation
- 1998-02-13 CZ CZ0285199A patent/CZ296543B6/cs not_active IP Right Cessation
- 1998-02-13 CN CN98802483A patent/CN1093128C/zh not_active Expired - Lifetime
- 1998-06-14 SA SA98190146A patent/SA98190146B1/ar unknown
-
1999
- 1999-08-10 BG BG103649A patent/BG63970B1/bg unknown
- 1999-08-13 OA OA9900180A patent/OA11086A/en unknown
- 1999-08-13 NO NO993912A patent/NO317761B1/no not_active IP Right Cessation
-
2000
- 2000-07-25 HK HK00104616A patent/HK1026206A1/xx not_active IP Right Cessation
-
2001
- 2001-08-14 US US09/929,604 patent/US6458963B1/en not_active Expired - Fee Related
-
2006
- 2006-02-14 CY CY0600005A patent/CY2551B1/xx unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant, registration |