CAS: 314771-76-1; (S)-N4-(3-Chloro-4-Fluorophenyl)-7-((Tetrahydrofuran-3-yl)Oxy)Quinazoline-4,6-Diamine

上下游产品

N-(3-氯-4-氟苯基)-6-硝基-7-[[(3S)-四氢-3-呋喃基]氧基]-4-喹唑啉胺 4-[(3-Chloro-4-Fluorophenyl)Amino]-6-Nitro-7-[(S)-(Tetrahydrofuran-3-yl)Oxy]Quinazoline 314771-88-5
4-[(3-Chloro-4-Fluorophenyl)Amino]-6-Nitro-7-(5-Tetrahydrofuran-3-Yloxy)Quinazoline
4-((3-Chloro-4-Fluorophenyl)Amino)-6-Nitroquinazolin-7-Ol
7-氯-N-(3-氯-4-氟苯基)-6-硝基-4-氨基喹唑啉 7-Chloro-N-(3-Chloro-4-Fluorophenyl)-6-Nitroquinazolin-4-Amine 179552-73-9
N-(3-氯-4-氟苯基)-7-氟-6-硝基-4-喹唑啉胺 N-(3-Chloro-4-Fluorophenyl)-7-Fluoro-6-Nitroquinazolin-4-Amine 162012-67-1
阿法替尼中间体 N-((3-Chloro-4-Fluorophenyl)-6-Nitro-7-Phenylsulfonyl)Quinazolin-4-One 945553-94-6
(S)-6 Nitro-7-((Tetrahydrofuran-3-yl)Oxy)Quinazolin-4(3H)-One 1621182-18-0

7-氯-N-(3-氯-4-氟苯基)-6-硝基-4-氨基喹唑啉置于iron(Iii) Chloride Hexahydrate,Potassium Tert-Butylate,甲烷,一水合肼体系中,用 乙醇,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 9.0H,反应生成 N4-(3-氯-4-氟苯基)-7-[[(3S)-四氢-3-呋喃基]氧基]-4,6-喹唑啉二胺
参考文献:一种阿法替尼合成工艺的改进方法
标题:一种阿法替尼合成工艺的改进方法
摘要:本发明公开了一种阿法替尼合成工艺的改进方法,属于有机合成的技术领域.本发明对阿法替尼合成工艺中氯化,胺化,醚化和还原反应进行了改进优化并提高了产品的收率及纯度,简化了工艺操作,降低了生产成本,后处理方便,干净,具有较高的实用性.相比于现有技术,本发明对阿法替尼制备方法的改进克服了诸多不足,收率高,步骤简单,总收率约为71%,纯度为98%.其主要优点是步骤简化,反应条件温和,操作简便,收率高以及纯度高等,有利于工业化生产.

专利信息

专利号:US-9242965-B2
优先权日:2013-12-31
标题:Process for the manufacture of (E)-4-N,N-dialkylamino crotonic acid in HX salt form and use thereof for synthesis of EGFR tyrosine kinase inhibitors
发明人：ZHENG JUNCHENG; DENG DA; LV GUANGHUA; YAN JUN; BRANDENBURG JOERG; KROEBER JUTTA; SCHOLZ ULRICH
权利人:BOEHRINGER INGELHEIM INT
摘要:The present invention is directed to an efficient process for the manufacture of (E)-4-N,N-dialkylamino crotonic acid in HX salt form of formula I n nwherein R 1 and R 2 independently denote C 1-3 -alkyl groups and X − denotes an acid anion, such as the chloride, bromide, tosylate, mesylate or trifluoroacetate anion, with high quality, and a process for synthesis of EGFR tyrosine kinase inhibitors with heterocyclic quinazoline, quinoline or pyrimidopyrimidine core structure, using the acid addition salt I and activated derivatives thereof as intermediates.

专利号:EP-3089961-B1
优先权日:2013-12-31
标 题:Process for the manufacture of (e)-4-n,n-dialkylamino crotonic acid in hx salt form and use thereof for synthesis of egfr tyrosine kinase inhibitors

专利号:EP-3089961-A1
优先权日:2013-12-31
标题 :Process for the manufacture of (e)-4-n,n-dialkylamino crotonic acid in hx salt form and use thereof for synthesis of egfr tyrosine kinase inhibitors

专利号:CN-114315595-B
优先权日:2021-11-30
标题 :Preparation method of a carbon-supported iron-based catalyst and its application in the synthesis of anti-cancer inhibitor intermediates

专利号:US-2015183764-A1
优先权日:2013-12-31
标 题 :Process for the manufacture of (e)-4-n,n-dialkylamino crotonic acid in hx salt form and use thereof for synthesis of egfr tyrosine kinase inhibitors

专利号:JP-6594333-B2
优先权日:2013-12-31
标 题:Process for the preparation of (E) -4-N, N-dialkylaminocrotonic acid in the form of an HX salt and its use for the synthesis of EGFR tyrosine kinase inhibitors