ES2151850B1 - Intermedio para la sintesis de amlodipino para su obtencion y utilizacion correspondiente. - Google Patents
Intermedio para la sintesis de amlodipino para su obtencion y utilizacion correspondiente.Info
- Publication number
- ES2151850B1 ES2151850B1 ES009802240A ES9802240A ES2151850B1 ES 2151850 B1 ES2151850 B1 ES 2151850B1 ES 009802240 A ES009802240 A ES 009802240A ES 9802240 A ES9802240 A ES 9802240A ES 2151850 B1 ES2151850 B1 ES 2151850B1
- Authority
- ES
- Spain
- Prior art keywords
- synthesis
- corresponding use
- chem
- preparation
- amlodipino
- Prior art date
- Legal status (The legal status 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 status listed.)
- Expired - Fee Related
Links
- HTIQEAQVCYTUBX-UHFFFAOYSA-N amlodipine Chemical compound CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1C1=CC=CC=C1Cl HTIQEAQVCYTUBX-UHFFFAOYSA-N 0.000 title abstract 2
- 230000015572 biosynthetic process Effects 0.000 title abstract 2
- 238000003786 synthesis reaction Methods 0.000 title abstract 2
- 238000000034 method Methods 0.000 abstract 3
- 238000002360 preparation method Methods 0.000 abstract 3
- USFZMSVCRYTOJT-UHFFFAOYSA-N Ammonium acetate Chemical compound N.CC(O)=O USFZMSVCRYTOJT-UHFFFAOYSA-N 0.000 abstract 1
- 239000005695 Ammonium acetate Substances 0.000 abstract 1
- WDJHALXBUFZDSR-UHFFFAOYSA-M acetoacetate Chemical compound CC(=O)CC([O-])=O WDJHALXBUFZDSR-UHFFFAOYSA-M 0.000 abstract 1
- 229960000528 amlodipine Drugs 0.000 abstract 1
- 229940043376 ammonium acetate Drugs 0.000 abstract 1
- 235000019257 ammonium acetate Nutrition 0.000 abstract 1
- 125000000649 benzylidene group Chemical group [H]C(=[*])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- OEBFVKDPQVFAPH-LUAWRHEFSA-N ethyl (z)-3-amino-4-[2-(1,3-dioxoisoindol-2-yl)ethoxy]but-2-enoate Chemical group C1=CC=C2C(=O)N(CCOCC(/N)=C/C(=O)OCC)C(=O)C2=C1 OEBFVKDPQVFAPH-LUAWRHEFSA-N 0.000 abstract 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/44—Iso-indoles; Hydrogenated iso-indoles
- C07D209/48—Iso-indoles; Hydrogenated iso-indoles with oxygen atoms in positions 1 and 3, e.g. phthalimide
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Heart & Thoracic Surgery (AREA)
- General Health & Medical Sciences (AREA)
- Vascular Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Urology & Nephrology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Cardiology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Indole Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Hydrogenated Pyridines (AREA)
- Solid-Sorbent Or Filter-Aiding Compositions (AREA)
- Electric Double-Layer Capacitors Or The Like (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Abstract
Intermedio para la síntesis del amlodipino, procedimiento para su obtención y utilización correspondiente. El intermedio es el 3- amino-4-(2-ftalimido)etoxi)crotonato de etilo y es de fórmula III **FÓRMULA 1** El procedimiento para su obtención comprende la reacción del acetoacetato de fórmula **FÓRMULA 2** con acetato amónico; y su utilización es para la preparación del compuesto de fórmula **FÓRMULA 3** llevándose a cabo mediante la reacción del 3-amino-4-(2-ftalimido)etoxi)crotonato de etilo con un benciliden derivado.
Priority Applications (13)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ES009802240A ES2151850B1 (es) | 1998-10-26 | 1998-10-26 | Intermedio para la sintesis de amlodipino para su obtencion y utilizacion correspondiente. |
| SI9930870T SI1125924T1 (sl) | 1998-10-26 | 1999-10-18 | Intermediat za sintezo amlodipina, postopek za pripravo in ustrezna uporaba |
| DE69929079T DE69929079T2 (de) | 1998-10-26 | 1999-10-18 | Zwischenstufe für die synthese von amlodipin, herstellungsverfahren und entsprechende anwendung |
| EP99952654A EP1125924B1 (en) | 1998-10-26 | 1999-10-18 | Intermediate for the synthesis of amlodipine, preparation process and corresponding utilization |
| DK99952654T DK1125924T3 (da) | 1998-10-26 | 1999-10-18 | Mellemprodukt til syntesen af amlodipin, fremstillingsfremgangsmåde og tilsvarende anvendelse |
| JP2000578284A JP2002528436A (ja) | 1998-10-26 | 1999-10-18 | アムロジピン合成用中間体、その調製方法および使用方法 |
| AT99952654T ATE313526T1 (de) | 1998-10-26 | 1999-10-18 | Zwischenstufe für die synthese von amlodipin, herstellungsverfahren und entsprechende anwendung |
| ES99952654T ES2251843T3 (es) | 1998-10-26 | 1999-10-18 | Intermedio para la sintesis del amlodipino, procedimiento para su obtencion y utilizacion correspondiente. |
| CA002349013A CA2349013C (en) | 1998-10-26 | 1999-10-18 | Intermediate for the synthesis of amlodipine, a process for the preparation thereof and corresponding use |
| AU64772/99A AU752042B2 (en) | 1998-10-26 | 1999-10-18 | Intermediate for the synthesis of amlodipine, preparation process and corresponding utilization |
| PCT/ES1999/000333 WO2000024714A1 (es) | 1998-10-26 | 1999-10-18 | Intermedio para la sintesis de amlodipino, procedimiento para su obtencion y utilizacion correspondiente |
| KR1020017005232A KR100576166B1 (ko) | 1998-10-26 | 1999-10-18 | 아믈로디핀 합성을 위한 중간체, 이의 제조 방법 및 이의용도 |
| US10/041,475 US6603006B2 (en) | 1998-10-26 | 2002-01-10 | Intermediate for the synthesis of amlodipine, a process for the preparation thereof and corresponding use |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ES009802240A ES2151850B1 (es) | 1998-10-26 | 1998-10-26 | Intermedio para la sintesis de amlodipino para su obtencion y utilizacion correspondiente. |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| ES2151850A1 ES2151850A1 (es) | 2001-01-01 |
| ES2151850B1 true ES2151850B1 (es) | 2001-08-16 |
Family
ID=8305582
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES009802240A Expired - Fee Related ES2151850B1 (es) | 1998-10-26 | 1998-10-26 | Intermedio para la sintesis de amlodipino para su obtencion y utilizacion correspondiente. |
| ES99952654T Expired - Lifetime ES2251843T3 (es) | 1998-10-26 | 1999-10-18 | Intermedio para la sintesis del amlodipino, procedimiento para su obtencion y utilizacion correspondiente. |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES99952654T Expired - Lifetime ES2251843T3 (es) | 1998-10-26 | 1999-10-18 | Intermedio para la sintesis del amlodipino, procedimiento para su obtencion y utilizacion correspondiente. |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US6603006B2 (es) |
| EP (1) | EP1125924B1 (es) |
| JP (1) | JP2002528436A (es) |
| KR (1) | KR100576166B1 (es) |
| AT (1) | ATE313526T1 (es) |
| AU (1) | AU752042B2 (es) |
| CA (1) | CA2349013C (es) |
| DE (1) | DE69929079T2 (es) |
| DK (1) | DK1125924T3 (es) |
| ES (2) | ES2151850B1 (es) |
| SI (1) | SI1125924T1 (es) |
| WO (1) | WO2000024714A1 (es) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR0116554A (pt) | 2000-12-29 | 2004-02-03 | Pfizer Ltd | Composto, composição farmacêutica para o tratamento da angina ou hipertensão, processo, processo para o tratamento ou prevenção da angina ou hipertensão, composição do ingrediente farmaceuticamente ativo e composição farmacêutica para o tratamento ou prevenção da angina ou hipertensão |
| CA2433181C (en) | 2000-12-29 | 2005-11-22 | Pfizer Limited | Amlodipine hemifumarate |
| DE60116514T2 (de) | 2000-12-29 | 2006-08-17 | Pfizer Ltd., Sandwich | Amlodipinhemimaleat |
| US7335380B2 (en) | 2000-12-29 | 2008-02-26 | Synthon Ip Inc. | Amlodipine free base |
| MXPA03005882A (es) | 2000-12-29 | 2005-04-19 | Pfizer Ltd | Derivado amida de amlodipina. |
| EP1309555B1 (en) | 2000-12-29 | 2005-07-27 | Pfizer Limited | Process for making amlodipine maleate |
| WO2002054062A2 (en) | 2000-12-29 | 2002-07-11 | Pfizer Limited | Reference standards and processes for determining the purity or stability of amlodipine maleate |
| BR0116553A (pt) | 2000-12-29 | 2004-02-03 | Pfizer Ltd | Composto, composição farmacêutica para tratamento de angina ou hipertensão, processo, processo para tratamento ou prevenção de angina ou hipertensão, composição de ingredientes farmaceuticamente ativos, composição farmacêutica para tratamento ou prevenção de angina ou hipertensão e processo para tratar ou prevenir angina ou hipertensão |
| US6653481B2 (en) | 2000-12-29 | 2003-11-25 | Synthon Bv | Process for making amlodipine |
| AT5874U1 (de) | 2000-12-29 | 2003-01-27 | Bioorg Bv | Pharmazeutische zubereitungen enthaltend amlodipinmaleat |
| US6680334B2 (en) | 2001-08-28 | 2004-01-20 | Pfizer Inc | Crystalline material |
| US6784297B2 (en) | 2002-09-04 | 2004-08-31 | Kopran Limited | Process for the preparation of anti-ischemic and anti-hypertensive drug amlodipine besylate |
| US20040072879A1 (en) * | 2002-10-10 | 2004-04-15 | Dr. Reddy's Laboratories Limited | Crystalline 2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-3-ethoxycarbonyl-5-methoxycarbonyl-6-methyl-1,4-dihydropyridine maleate salt (Amlodipine) |
| ES2211317B1 (es) * | 2002-11-18 | 2005-10-16 | Finaf 92, S.A. | Compuestos intermedios para la obtencion de principios activos antihipertensivos y procedimientos correspondientes. |
| AU2004218241B2 (en) * | 2003-03-07 | 2010-06-03 | Syngenta Participations Ag | Process for the production of substituted nicotinic acid esters |
| KR100807336B1 (ko) | 2006-10-23 | 2008-02-28 | 명문제약주식회사 | 암로디핀의 제조를 위한 신규한 중간체 화합물, 이의 제조방법 및 이를 이용한 암로디핀의 제조 방법 |
| JP2010100562A (ja) * | 2008-10-23 | 2010-05-06 | Daito Kk | アムロジピン製造中間体の精製方法 |
| EP3334485B1 (en) | 2015-08-14 | 2024-03-06 | ResMed Pty Ltd | Monitoring respiratory pressure therapy |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CS228917B2 (en) * | 1981-03-14 | 1984-05-14 | Pfizer | Method of preparing substituted derivatives of 1,4-dihydropyridine |
| DK161312C (da) * | 1982-03-11 | 1991-12-09 | Pfizer | Analogifremgangsmaade til fremstilling af 2-aminoalkoxymethyl-4-phenyl-6-methyl-1,4-dihydropyridin-3,5-dicarboxylsyreestere eller syreadditionssalte deraf samt phthalimidoderivater til anvendelse som udgangsmateriale ved fremgangsmaaden |
| PT77842B (en) * | 1982-12-21 | 1986-05-05 | Pfizer | Process for preparing dihydropyridines |
| GB8422139D0 (en) * | 1984-09-01 | 1984-10-03 | Fisons Plc | Biologically active nitrogen heterocyclics |
| AU7810087A (en) * | 1986-08-14 | 1988-03-08 | Byk Gulden Lomberg Chemische Fabrik Gmbh | New piperidines |
| GB9119983D0 (en) * | 1991-09-19 | 1991-11-06 | Erba Carlo Spa | Dihydropyridine derivatives useful in antitumor therapy |
-
1998
- 1998-10-26 ES ES009802240A patent/ES2151850B1/es not_active Expired - Fee Related
-
1999
- 1999-10-18 EP EP99952654A patent/EP1125924B1/en not_active Expired - Lifetime
- 1999-10-18 AU AU64772/99A patent/AU752042B2/en not_active Ceased
- 1999-10-18 DK DK99952654T patent/DK1125924T3/da active
- 1999-10-18 AT AT99952654T patent/ATE313526T1/de not_active IP Right Cessation
- 1999-10-18 ES ES99952654T patent/ES2251843T3/es not_active Expired - Lifetime
- 1999-10-18 JP JP2000578284A patent/JP2002528436A/ja active Pending
- 1999-10-18 DE DE69929079T patent/DE69929079T2/de not_active Expired - Lifetime
- 1999-10-18 KR KR1020017005232A patent/KR100576166B1/ko not_active Expired - Fee Related
- 1999-10-18 CA CA002349013A patent/CA2349013C/en not_active Expired - Fee Related
- 1999-10-18 WO PCT/ES1999/000333 patent/WO2000024714A1/es not_active Ceased
- 1999-10-18 SI SI9930870T patent/SI1125924T1/sl unknown
-
2002
- 2002-01-10 US US10/041,475 patent/US6603006B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| DE69929079D1 (de) | 2006-01-26 |
| ATE313526T1 (de) | 2006-01-15 |
| CA2349013C (en) | 2007-10-02 |
| ES2251843T3 (es) | 2006-05-01 |
| KR20010093781A (ko) | 2001-10-29 |
| DE69929079T2 (de) | 2006-06-22 |
| JP2002528436A (ja) | 2002-09-03 |
| EP1125924A1 (en) | 2001-08-22 |
| CA2349013A1 (en) | 2000-05-04 |
| ES2151850A1 (es) | 2001-01-01 |
| SI1125924T1 (sl) | 2006-04-30 |
| AU6477299A (en) | 2000-05-15 |
| KR100576166B1 (ko) | 2006-05-03 |
| WO2000024714A1 (es) | 2000-05-04 |
| DK1125924T3 (da) | 2006-05-08 |
| EP1125924B1 (en) | 2005-12-21 |
| US20020068831A1 (en) | 2002-06-06 |
| AU752042B2 (en) | 2002-09-05 |
| US6603006B2 (en) | 2003-08-05 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EC2A | Search report published |
Date of ref document: 20010101 Kind code of ref document: A1 Effective date: 20010101 |
|
| FD2A | Announcement of lapse in spain |
Effective date: 20180807 |