摘要
报道一条制备盐酸厄洛替尼的新路线。以4,5-二甲氧基乙氧基-2-胺基苯甲腈为原料,经环合反应制得关键中间体6,7-二(2-甲氧基乙氧基)喹唑啉-4-胺(2);2经钯催化的Buchwald-Hartwig偶联、水解和Best-mann-Ohira反应后成盐合成了盐酸厄洛替尼,总收率34%。其结构经1H NMR和ESI-HR-MS确认。
A new synthetic route for preparation of Erlotinib hydrochloride was reported.A key intermediate,6,7-bis（2-methoxyethoxy）quinazolin-4-amine（2）,was prepared by cyclization of 2-amino-4,5-bis（2-methoxyethoxy）benzonitrile.Erlotinib hydrochloride in total yield of 34% was synthesized from 2 by Pd-catalyzed Buchwald-Hartwig cross-coupling reaction,hydrolysis and Bestmann-Ohira reaction,then saltforming.The structures were confirmed by 1H NMR and ESI-HR-MS.
出处
《合成化学》
CAS
CSCD
北大核心
2013年第4期505-507,512,共4页
Chinese Journal of Synthetic Chemistry
