JP2012524769A - ４−（３−クロロ−２−フルオロアニリノ）−７−メトキシ−６−｛［１−（ｎ−メチルカルバモイルメチル）ピペリジン−４−イル］オキシ｝キナゾリンの製造方法 - Google Patents

４−（３−クロロ−２−フルオロアニリノ）−７−メトキシ−６−｛［１−（ｎ−メチルカルバモイルメチル）ピペリジン−４−イル］オキシ｝キナゾリンの製造方法 Download PDF

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JP2012524769A
JP2012524769A JP2012506579A JP2012506579A JP2012524769A JP 2012524769 A JP2012524769 A JP 2012524769A JP 2012506579 A JP2012506579 A JP 2012506579A JP 2012506579 A JP2012506579 A JP 2012506579A JP 2012524769 A JP2012524769 A JP 2012524769A
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Prior art keywords
compound
formula
chloro
acid
iii
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Japanese (ja)
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JP2012524769A5 (enExample
Inventor
ボードマン，ケイ・アリソン
カニンガム，オリバー・ロバート
ゴウンドリー，ウィリアム
ラファン，デヴィッド・ダーモット・パトリック
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AstraZeneca AB
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AstraZeneca AB
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Publication of JP2012524769A publication Critical patent/JP2012524769A/ja
Publication of JP2012524769A5 publication Critical patent/JP2012524769A5/ja
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    • 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

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  • 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)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Hydrogenated Pyridines (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
JP2012506579A 2009-04-23 2010-04-22 ４−（３−クロロ−２−フルオロアニリノ）−７−メトキシ−６−｛［１−（ｎ−メチルカルバモイルメチル）ピペリジン−４−イル］オキシ｝キナゾリンの製造方法 Pending JP2012524769A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US17199409P 2009-04-23 2009-04-23
US61/171,994 2009-04-23
PCT/GB2010/050653 WO2010122340A2 (en) 2009-04-23 2010-04-22 Process 738

Publications (2)

Publication Number Publication Date
JP2012524769A true JP2012524769A (ja) 2012-10-18
JP2012524769A5 JP2012524769A5 (enExample) 2013-05-02

Family

ID=42224659

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JP2012506579A Pending JP2012524769A (ja) 2009-04-23 2010-04-22 ４−（３−クロロ−２−フルオロアニリノ）−７−メトキシ−６−｛［１−（ｎ−メチルカルバモイルメチル）ピペリジン−４−イル］オキシ｝キナゾリンの製造方法

Country Status (14)

Country Link
US (1) US8450482B2 (enExample)
EP (1) EP2421827A2 (enExample)
JP (1) JP2012524769A (enExample)
KR (1) KR20120007059A (enExample)
CN (1) CN102459174A (enExample)
AR (1) AR076407A1 (enExample)
AU (1) AU2010240717A1 (enExample)
BR (1) BRPI1013854A2 (enExample)
CA (1) CA2758610A1 (enExample)
IL (1) IL215388A0 (enExample)
MX (1) MX2011011177A (enExample)
SG (1) SG174893A1 (enExample)
TW (1) TW201041871A (enExample)
WO (1) WO2010122340A2 (enExample)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
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

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005023783A1 (en) * 2003-09-05 2005-03-17 Astrazeneca Ab Process for the manufacture of gefitinib
WO2005115145A2 (en) * 2004-05-20 2005-12-08 Wyeth Quinone substituted quinazoline and quinoline kinase inhibitors
JP2007505875A (ja) * 2003-09-19 2007-03-15 アストラゼネカ アクチボラグ キナゾリン誘導体
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
JP2011520857A (ja) * 2008-05-13 2011-07-21 アストラゼネカ アクチボラグ ４−（３−クロロ−２−フルオロアニリノ）−７−メトキシ−６−｛［１−（ｎ−メチルカルバモイルメチル）ピペリジン−４−イル］オキシ｝キナゾリンのフマル酸塩

Family Cites Families (2)

* Cited by examiner, † Cited by third party
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

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005023783A1 (en) * 2003-09-05 2005-03-17 Astrazeneca Ab Process for the manufacture of gefitinib
JP2007505875A (ja) * 2003-09-19 2007-03-15 アストラゼネカ アクチボラグ キナゾリン誘導体
WO2005115145A2 (en) * 2004-05-20 2005-12-08 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
JP2011520857A (ja) * 2008-05-13 2011-07-21 アストラゼネカ アクチボラグ ４−（３−クロロ−２−フルオロアニリノ）−７−メトキシ−６−｛［１−（ｎ−メチルカルバモイルメチル）ピペリジン−４−イル］オキシ｝キナゾリンのフマル酸塩

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
"Appl.No:903/CHE/2006A", PATENT APPLICATION PUBLICATION 及び COMPLETE SPECIFICATION, JPN7014001385, 30 June 2006 (2006-06-30), pages , ISSN: 0002807504 *

Also Published As

Publication number Publication date
WO2010122340A8 (en) 2011-12-15
SG174893A1 (en) 2011-11-28
EP2421827A2 (en) 2012-02-29
AU2010240717A1 (en) 2011-10-27
AR076407A1 (es) 2011-06-08
MX2011011177A (es) 2011-11-18
TW201041871A (en) 2010-12-01
IL215388A0 (en) 2011-12-29
WO2010122340A3 (en) 2011-09-09
KR20120007059A (ko) 2012-01-19
CN102459174A (zh) 2012-05-16
US20120108814A1 (en) 2012-05-03
US8450482B2 (en) 2013-05-28
BRPI1013854A2 (pt) 2017-05-16
CA2758610A1 (en) 2010-10-28
WO2010122340A2 (en) 2010-10-28

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