摘要
4-氯-7-氟喹唑啉通过硝化制得4-氯-7-氟-6-硝基喹唑啉,再经与3-氯-4-氟苯胺缩合、与3-(4-吗啉基)-1-丙醇取代,用三氟乙酸乙酯进行氨基保护还原、RaneyNi催化氢化,然后与丙烯酸缩合、脱保护即得抗肿瘤药卡奈替尼,总收率约70%。
Canertinib, an antitumor agent, was synthesized from 4-chloro-7-fluoroquinazoline by nitration to give 4-chloro-7-fluoro-6-nitroquinazoline, which was subjected to condensation with 3-chloro-4-fluoroaniline, substitution with 3-（morpholin-4-yl）-1-propanol, protection with ethyl trifluoroacetate, reduction by hydrogen catalized by Raney Ni, condensation with propenoic acid, and then deprotection with potassium carbonate with an overall yield of about 70 %.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2010年第6期404-406,409,共4页
Chinese Journal of Pharmaceuticals
关键词
卡奈替尼
抗肿瘤药
合成
canertinib
antitumor agent
synthesis
