AR076407A1 - Un proceso para la preparacion de 4-(3-cloro-2-fluoroanilino)-7-metoxi-6-{[1-(n-metilcarbamilmetil)piperidin-4-il]oxi}quinazolina e intermediarios utilizados en el mismo. - Google Patents
Un proceso para la preparacion de 4-(3-cloro-2-fluoroanilino)-7-metoxi-6-{[1-(n-metilcarbamilmetil)piperidin-4-il]oxi}quinazolina e intermediarios utilizados en el mismo.Info
- Publication number
- AR076407A1 AR076407A1 ARP100101374A ARP100101374A AR076407A1 AR 076407 A1 AR076407 A1 AR 076407A1 AR P100101374 A ARP100101374 A AR P100101374A AR P100101374 A ARP100101374 A AR P100101374A AR 076407 A1 AR076407 A1 AR 076407A1
- Authority
- AR
- Argentina
- Prior art keywords
- chloro
- formula
- fluoroanilino
- quinazoline
- piperidin
- Prior art date
Links
- -1 3-CHLORO-2-FLUOROANILINO Chemical class 0.000 title abstract 3
- 238000000034 method Methods 0.000 title abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 5
- 150000003839 salts Chemical class 0.000 abstract 4
- 239000002253 acid Substances 0.000 abstract 2
- 125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 abstract 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 2
- 125000006239 protecting group Chemical group 0.000 abstract 2
- XWBTZHDDWRNOQH-UHFFFAOYSA-N 3-chloro-2-fluoroaniline Chemical compound NC1=CC=CC(Cl)=C1F XWBTZHDDWRNOQH-UHFFFAOYSA-N 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
Classifications
-
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C257/00—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines
- C07C257/10—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines
- C07C257/12—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines having carbon atoms of amidino groups bound to hydrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
- C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
- C07D211/40—Oxygen atoms
- C07D211/44—Oxygen atoms attached in position 4
- C07D211/46—Oxygen atoms attached in position 4 having a hydrogen atom as the second substituent in position 4
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Hydrogenated Pyridines (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Procesos para preparar 4-(3-cloro-2-fluoroanilino)-7-metoxi-6-{[1-(N-metilcarbamilmetil)piperidin-4-il]oxi}quinazolina y sales de esta, e intermediarios usados en el proceso. Reivindicacion 1: Un proceso para preparar 4-(3-cloro-2-fluoroanilino)-7-metoxi-6-{[1-(N-metilcarbamilmetil)piperidin-4-il]oxi}quinazolina o una sal de ésta, caracterizado porque comprende (a) hacer reaccionar un compuesto de formula (2) con 3-cloro-2-fluoroanilina, en presencia de un ácido apropiado; o (b) hacer reaccionar un compuesto de formula (3)con un compuesto de formula (9) o de formula (12) en presencia de un ácido apropiado. Reivindicacion 9: Un compuesto, caracterizado porque es de formula (13) o una sal del mismo donde R1 es H, -NH2, -NO2, -N=C-N(CH3)2; R2 es H, N-metilcarbamoilmetilo, o Pg1, y Pg1 es un grupo protector de amino; con la condicion de que cuando R2 es H o un grupo protector de amino entonces R1 es H. Reivindicacion 12: Un compuesto, caracterizado porque es de formula (11), formula (12) o una sal del mismo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US17199409P | 2009-04-23 | 2009-04-23 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR076407A1 true AR076407A1 (es) | 2011-06-08 |
Family
ID=42224659
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP100101374A AR076407A1 (es) | 2009-04-23 | 2010-04-23 | Un proceso para la preparacion de 4-(3-cloro-2-fluoroanilino)-7-metoxi-6-{[1-(n-metilcarbamilmetil)piperidin-4-il]oxi}quinazolina e intermediarios utilizados en el mismo. |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US8450482B2 (es) |
| EP (1) | EP2421827A2 (es) |
| JP (1) | JP2012524769A (es) |
| KR (1) | KR20120007059A (es) |
| CN (1) | CN102459174A (es) |
| AR (1) | AR076407A1 (es) |
| AU (1) | AU2010240717A1 (es) |
| BR (1) | BRPI1013854A2 (es) |
| CA (1) | CA2758610A1 (es) |
| IL (1) | IL215388A0 (es) |
| MX (1) | MX2011011177A (es) |
| SG (1) | SG174893A1 (es) |
| TW (1) | TW201041871A (es) |
| WO (1) | WO2010122340A2 (es) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR101272613B1 (ko) | 2011-10-05 | 2013-06-10 | 한미사이언스 주식회사 | 1-(4-(4-(3,4-디클로로-2-플루오로페닐아미노)-7-메톡시퀴나졸린-6-일옥시)피페리딘-1-일)프로프-2-엔-1-온 염산염의 제조 방법 및 이에 사용되는 중간체 |
| CN108503596A (zh) * | 2018-03-14 | 2018-09-07 | 盐城师范学院 | 一种新的厄洛替尼及其中间体的制备方法 |
| CN108440420A (zh) * | 2018-03-22 | 2018-08-24 | 盐城师范学院 | 酪氨酸激酶抑制剂拉帕替尼及其关键中间体的制备方法 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI324597B (en) | 2002-03-28 | 2010-05-11 | Astrazeneca Ab | Quinazoline derivatives |
| US6924285B2 (en) | 2002-03-30 | 2005-08-02 | Boehringer Ingelheim Pharma Gmbh & Co. | Bicyclic heterocyclic compounds, pharmaceutical compositions containing these compounds, their use and process for preparing them |
| GB0320793D0 (en) | 2003-09-05 | 2003-10-08 | Astrazeneca Ab | Chemical process |
| US8318752B2 (en) * | 2003-09-19 | 2012-11-27 | Astrazeneca Ab | 4-(3-chloro-2-fluoroanilino)-7-methoxy-6-{[1-(N-methylcarbamoyl-methyl)piperidin-4-yl]oxy}quinazoline, its pharmaceutically acceptable salts, and pharmaceutical compositions comprising the same |
| US20070299092A1 (en) * | 2004-05-20 | 2007-12-27 | Wyeth | Quinone Substituted Quinazoline and Quinoline Kinase Inhibitors |
| WO2009138779A1 (en) * | 2008-05-13 | 2009-11-19 | Astrazeneca Ab | Combination comprising 4- (3-chloro-2-fluoroanilino) -7-meth0xy-6- { [1- (n-methylcarbamoylmethyl) piperidin- 4-yl] oxyjquinazoline |
| MY183041A (en) * | 2008-05-13 | 2021-02-08 | Astrazeneca Ab | Fumarate salt of 4- (3-chloro-2-fluoroanilino) -7-methoxy-6- {[1- (n-methylcarbamoylmethyl) piperidin- 4-yl] oxy}quinazoline |
-
2010
- 2010-04-22 CN CN2010800288080A patent/CN102459174A/zh active Pending
- 2010-04-22 KR KR1020117027878A patent/KR20120007059A/ko not_active Withdrawn
- 2010-04-22 MX MX2011011177A patent/MX2011011177A/es not_active Application Discontinuation
- 2010-04-22 US US13/264,217 patent/US8450482B2/en not_active Expired - Fee Related
- 2010-04-22 EP EP10715333A patent/EP2421827A2/en not_active Withdrawn
- 2010-04-22 AU AU2010240717A patent/AU2010240717A1/en not_active Abandoned
- 2010-04-22 CA CA2758610A patent/CA2758610A1/en not_active Abandoned
- 2010-04-22 JP JP2012506579A patent/JP2012524769A/ja active Pending
- 2010-04-22 WO PCT/GB2010/050653 patent/WO2010122340A2/en not_active Ceased
- 2010-04-22 BR BRPI1013854A patent/BRPI1013854A2/pt not_active IP Right Cessation
- 2010-04-22 SG SG2011068426A patent/SG174893A1/en unknown
- 2010-04-23 TW TW099112893A patent/TW201041871A/zh unknown
- 2010-04-23 AR ARP100101374A patent/AR076407A1/es not_active Application Discontinuation
-
2011
- 2011-09-26 IL IL215388A patent/IL215388A0/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| BRPI1013854A2 (pt) | 2017-05-16 |
| WO2010122340A8 (en) | 2011-12-15 |
| SG174893A1 (en) | 2011-11-28 |
| CA2758610A1 (en) | 2010-10-28 |
| IL215388A0 (en) | 2011-12-29 |
| JP2012524769A (ja) | 2012-10-18 |
| KR20120007059A (ko) | 2012-01-19 |
| AU2010240717A1 (en) | 2011-10-27 |
| EP2421827A2 (en) | 2012-02-29 |
| TW201041871A (en) | 2010-12-01 |
| US8450482B2 (en) | 2013-05-28 |
| CN102459174A (zh) | 2012-05-16 |
| WO2010122340A3 (en) | 2011-09-09 |
| WO2010122340A2 (en) | 2010-10-28 |
| US20120108814A1 (en) | 2012-05-03 |
| MX2011011177A (es) | 2011-11-18 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |