BRPI0409154A - processo para a preparação de 5-(haloacetil)-8-(óxi substituìdo)-(1h)-quinolin-2-onas - Google Patents
processo para a preparação de 5-(haloacetil)-8-(óxi substituìdo)-(1h)-quinolin-2-onasInfo
- Publication number
- BRPI0409154A BRPI0409154A BRPI0409154-0A BRPI0409154A BRPI0409154A BR PI0409154 A BRPI0409154 A BR PI0409154A BR PI0409154 A BRPI0409154 A BR PI0409154A BR PI0409154 A BRPI0409154 A BR PI0409154A
- Authority
- BR
- Brazil
- Prior art keywords
- quinolin
- acetyl
- hydroxy
- substituted
- oxy
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
- C07D215/20—Oxygen atoms
- C07D215/24—Oxygen atoms attached in position 8
- C07D215/26—Alcohols; Ethers thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/08—Bronchodilators
-
- 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
-
- B—PERFORMING OPERATIONS; TRANSPORTING
- B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
- B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
- B01J31/00—Catalysts comprising hydrides, coordination complexes or organic compounds
- B01J31/02—Catalysts comprising hydrides, coordination complexes or organic compounds containing organic compounds or metal hydrides
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
-
- 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)
- Chemical Kinetics & Catalysis (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pulmonology (AREA)
- Materials Engineering (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Quinoline Compounds (AREA)
- Transition And Organic Metals Composition Catalysts For Addition Polymerization (AREA)
Abstract
"PROCESSO PARA A PREPARAçãO DE 5-(HALOACETIL)-8-(óXI SUBSTITUìDO)-(1H)-QUINOLIN-2-ONAS". A invenção refere-se a um processo para preparar 5-(<244>-haloacetil)-8-oxi substituído-(1H)-quinolin-2-onas. O processo envolve (i) reagir (a) 8-hidróxi-(1H)-quinolin-2-ona com um agente de acilação e um ácido Lewis para formar 5-acetil-8-hidróxi-(1H)-quinolin-2-ona; ou (b) 8-hidróxi-(1H)-quinolin-2-ona com um ácido Lewis para formar 5-acetil-8-hidróxi-(1H)-quinolin-2-ona; ou (c) 8-acetóxi-(1H)-quinolin-2-ona com um ácido Lewis para formar 5-acetil-8-hidróxi-(1H)-quinolin-2-ona; (ii) reagir o 5-acetil-8-hidróxi-(1H)-quinolin-2-ona preparado na Etapa (i) com um composto tendo a Fórmula RL na presença de uma base e um solvente para formar 5-acetil-8-oxi substituído(1H)-quinolin-2-ona, onde R é um grupo de proteção e L é um grupo de partida; e (iii) reagir o 5-acetil-8-oxi substituído-(1H)-quinolin-2-ona com um agente de halogenação na presença de um solvente para formar um 5-(<244>-haloacetil)-8-oxi substituído-(1H)-quinolin-2-ona.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US45972403P | 2003-04-02 | 2003-04-02 | |
| US60/459.724 | 2003-04-02 | ||
| PCT/EP2004/003479 WO2004087668A1 (en) | 2003-04-02 | 2004-04-01 | A process for the preparation of 5-(haloacetyl)-8-(substituted oxy)-(1h)-quinolin-2-ones |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| BRPI0409154A true BRPI0409154A (pt) | 2006-03-28 |
| BRPI0409154B1 BRPI0409154B1 (pt) | 2014-03-25 |
Family
ID=33131902
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0409154-0B1A BRPI0409154B1 (pt) | 2003-04-02 | 2004-04-01 | Processo para preparar 5-(alfa-haloacetil)-8-benzilóxi-(1H)-quinolin-2- onas |
Country Status (35)
| Country | Link |
|---|---|
| US (1) | US7605267B2 (pt) |
| EP (1) | EP1613599B8 (pt) |
| JP (1) | JP4726778B2 (pt) |
| KR (1) | KR101073740B1 (pt) |
| CN (1) | CN1774423A (pt) |
| AR (2) | AR043825A1 (pt) |
| AT (1) | ATE491690T1 (pt) |
| AU (1) | AU2004226212B2 (pt) |
| BR (1) | BRPI0409154B1 (pt) |
| CA (1) | CA2520990C (pt) |
| CL (1) | CL2004000706A1 (pt) |
| CO (1) | CO5700779A2 (pt) |
| CY (1) | CY1111515T1 (pt) |
| DE (1) | DE602004030553D1 (pt) |
| DK (1) | DK1613599T3 (pt) |
| EC (1) | ECSP056059A (pt) |
| ES (1) | ES2358193T3 (pt) |
| HK (1) | HK1086833A1 (pt) |
| HR (1) | HRP20110184T1 (pt) |
| IL (1) | IL171053A (pt) |
| IS (1) | IS2800B (pt) |
| MA (1) | MA27761A1 (pt) |
| MX (1) | MXPA05010616A (pt) |
| MY (1) | MY141871A (pt) |
| NO (1) | NO331980B1 (pt) |
| NZ (1) | NZ542623A (pt) |
| PE (2) | PE20050211A1 (pt) |
| PL (1) | PL1613599T3 (pt) |
| PT (1) | PT1613599E (pt) |
| RU (1) | RU2339621C2 (pt) |
| SI (1) | SI1613599T1 (pt) |
| TN (1) | TNSN05245A1 (pt) |
| TW (1) | TWI324151B (pt) |
| WO (1) | WO2004087668A1 (pt) |
| ZA (1) | ZA200507603B (pt) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0411056D0 (en) | 2004-05-18 | 2004-06-23 | Novartis Ag | Organic compounds |
| GB0413960D0 (en) * | 2004-06-22 | 2004-07-28 | Novartis Ag | Organic compounds |
| ES2396987T3 (es) | 2006-06-30 | 2013-03-01 | Novartis Ag | Derivados de quinolina y sus composiciones farmacéuticas |
| WO2013132514A2 (en) * | 2012-03-09 | 2013-09-12 | Rao Davuluri Ramamohan | A novel process for the preparation of (r)-5-[2-[(5, 6-diethyl-2, 3-dihydro-1h-inden-2-yl) amino]-1-hydroxyethyl]-8-hydroxy quinolin-2(1h)-one |
| CN102633717B (zh) * | 2012-03-30 | 2013-11-20 | 西南大学 | N-乙酰-喹啉-2(1h)酮类化合物及其制备方法和应用 |
| CN104379566B (zh) * | 2012-07-11 | 2016-08-24 | 上海威智医药科技有限公司 | 茚达特罗中间体及茚达特罗的合成方法 |
| CZ306252B6 (cs) | 2013-03-15 | 2016-10-26 | Zentiva, K.S. | Způsob přípravy 5-[(R)-2-(5,6-diethylindan-2-ylamino)-1-hydroxyethyl]-8-hydroxy-(1H)-chinolin-2-onu (indacaterolu) |
| EP3092217B1 (en) | 2014-01-09 | 2020-06-03 | Davuluri, Ramamohan Rao | A novel process for preparation of indacaterol or its pharmaceutically acceptable salts |
| CN105693603B (zh) * | 2014-11-24 | 2019-11-29 | 上海医药工业研究院 | 改良的马来酸茚达特罗制备工艺 |
| CN107531636B (zh) * | 2015-04-09 | 2022-11-25 | 正大天晴药业集团股份有限公司 | 茚达特罗或其盐的制备方法 |
| CN107868045A (zh) * | 2016-09-28 | 2018-04-03 | 四川海思科制药有限公司 | 一种茚达特罗中间体的制备方法 |
| CN108264483A (zh) * | 2016-12-31 | 2018-07-10 | 天津金耀集团有限公司 | 一种马来酸茚达特罗的制备方法 |
| CN109721534B (zh) * | 2018-09-25 | 2022-05-20 | 四川海思科制药有限公司 | 一种马来酸茚达特罗中间体及其制备方法和用途 |
| CN114751857A (zh) * | 2022-04-29 | 2022-07-15 | 梯尔希（南京）药物研发有限公司 | 一种茚达特罗杂质的制备方法 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS539228B2 (pt) * | 1974-01-31 | 1978-04-04 | ||
| CA1164459A (en) | 1980-11-11 | 1984-03-27 | Yung-Hsiung Yang | Process for preparing (imidazo¬1,2-a|pyridine- 2-yl)-carbostyril or -3,4-dihydrocarbostyryl derivatives |
| JPS5896022A (ja) * | 1981-11-30 | 1983-06-07 | Otsuka Pharmaceut Co Ltd | 強心剤 |
| ES8403457A1 (es) * | 1983-01-28 | 1984-03-16 | Espanola Farma Therapeut | Procedimiento para la obtencion de un compuesto derivado de la 2-quinolinona. |
| ES8605239A1 (es) | 1985-12-04 | 1986-03-16 | Astur Pharma | Un procedimiento para la preparacion de quinolonas sustitui-das |
| GB9405019D0 (en) * | 1994-03-15 | 1994-04-27 | Smithkline Beecham Plc | Novel compounds |
| GB9913083D0 (en) * | 1999-06-04 | 1999-08-04 | Novartis Ag | Organic compounds |
| GB0029562D0 (en) * | 2000-12-04 | 2001-01-17 | Novartis Ag | Organic compounds |
| WO2003042160A1 (en) * | 2001-11-13 | 2003-05-22 | Theravance, Inc. | Aryl aniline beta-2 adrenergic receptor agonists |
| TWI324150B (en) * | 2003-02-28 | 2010-05-01 | Novartis Ag | Process for preparing 5-[(r)-2-(5,6-diethyl-indan-2-ylamino)-1-hydroxy-ethyl]-8-hydroxy-(1h)-quinolin-2-one salt |
-
2004
- 2004-03-31 PE PE2004000341A patent/PE20050211A1/es not_active Application Discontinuation
- 2004-03-31 PE PE2010000225A patent/PE20100399A1/es not_active Application Discontinuation
- 2004-03-31 TW TW093108942A patent/TWI324151B/zh not_active IP Right Cessation
- 2004-04-01 SI SI200431618T patent/SI1613599T1/sl unknown
- 2004-04-01 CA CA2520990A patent/CA2520990C/en not_active Expired - Lifetime
- 2004-04-01 DE DE602004030553T patent/DE602004030553D1/de not_active Expired - Lifetime
- 2004-04-01 AT AT04725035T patent/ATE491690T1/de active
- 2004-04-01 DK DK04725035.2T patent/DK1613599T3/da active
- 2004-04-01 PT PT04725035T patent/PT1613599E/pt unknown
- 2004-04-01 RU RU2005133664/04A patent/RU2339621C2/ru active
- 2004-04-01 CN CNA2004800089560A patent/CN1774423A/zh active Pending
- 2004-04-01 US US10/550,621 patent/US7605267B2/en active Active
- 2004-04-01 WO PCT/EP2004/003479 patent/WO2004087668A1/en active Application Filing
- 2004-04-01 PL PL04725035T patent/PL1613599T3/pl unknown
- 2004-04-01 JP JP2006504953A patent/JP4726778B2/ja not_active Expired - Lifetime
- 2004-04-01 EP EP04725035A patent/EP1613599B8/en not_active Expired - Lifetime
- 2004-04-01 CL CL200400706A patent/CL2004000706A1/es unknown
- 2004-04-01 MY MYPI20041213A patent/MY141871A/en unknown
- 2004-04-01 NZ NZ542623A patent/NZ542623A/en not_active IP Right Cessation
- 2004-04-01 BR BRPI0409154-0B1A patent/BRPI0409154B1/pt not_active IP Right Cessation
- 2004-04-01 AR ARP040101105A patent/AR043825A1/es not_active Application Discontinuation
- 2004-04-01 MX MXPA05010616A patent/MXPA05010616A/es active IP Right Grant
- 2004-04-01 ES ES04725035T patent/ES2358193T3/es not_active Expired - Lifetime
- 2004-04-01 AU AU2004226212A patent/AU2004226212B2/en not_active Expired
-
2005
- 2005-09-20 ZA ZA200507603A patent/ZA200507603B/en unknown
- 2005-09-22 IL IL171053A patent/IL171053A/en active IP Right Grant
- 2005-09-29 EC EC2005006059A patent/ECSP056059A/es unknown
- 2005-09-30 KR KR1020057018750A patent/KR101073740B1/ko active IP Right Grant
- 2005-09-30 TN TNP2005000245A patent/TNSN05245A1/en unknown
- 2005-10-11 MA MA28545A patent/MA27761A1/fr unknown
- 2005-10-12 CO CO05104250A patent/CO5700779A2/es active IP Right Grant
- 2005-10-27 IS IS8095A patent/IS2800B/is unknown
- 2005-11-01 NO NO20055099A patent/NO331980B1/no unknown
-
2006
- 2006-06-16 HK HK06106919.9A patent/HK1086833A1/xx not_active IP Right Cessation
-
2011
- 2011-03-14 CY CY20111100284T patent/CY1111515T1/el unknown
- 2011-03-14 HR HR20110184T patent/HRP20110184T1/hr unknown
-
2016
- 2016-01-25 AR ARP160100188A patent/AR103508A2/es unknown
Also Published As
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B06F | Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette] | ||
| B15K | Others concerning applications: alteration of classification |
Free format text: PARA INT.CL: C07D 215/26, A61P 11/00 Ipc: C07D 215/26 (2011.01) |
|
| B07A | Application suspended after technical examination (opinion) [chapter 7.1 patent gazette] | ||
| B09A | Decision: intention to grant [chapter 9.1 patent gazette] | ||
| B16A | Patent or certificate of addition of invention granted [chapter 16.1 patent gazette] |
Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 01/04/2004, OBSERVADAS AS CONDICOES LEGAIS. |
|
| B21F | Lapse acc. art. 78, item iv - on non-payment of the annual fees in time |
Free format text: REFERENTE A 16A ANUIDADE. |
|
| B24J | Lapse because of non-payment of annual fees (definitively: art 78 iv lpi, resolution 113/2013 art. 12) |
Free format text: REFERENTE AO DESPACHO 21.6 PUBLICADO NA RPI 2560 DE 2020-01-28 |