N-(2-氨基苯基)-2-喹唑啉酮乙酰胺盐酸盐的合成

摘要

本文通过2-溴-N-(2-硝基苯)乙酰胺和取代的喹唑啉酮在NaH催化下发生亲核取代反应,再经过氢化、酸化合成了4个新型常山碱类抗球虫药物-N-(2-氨基苯基)-2-喹唑啉酮乙酰胺盐酸盐(1:1).其中,2-溴-N-(2-硝基苯)乙酰胺通过溴乙酰氯与邻硝基苯胺反应制备,取代的喹唑啉酮使用取代的邻氨基苯甲酸与甲酰胺反应合成.所有目标化合物的结构均经1 H NMR,IR和HRMS等方法确证.%Four novel N-(2~aminophenyl)-2-quinazolinone-acetamide hydrochloride ( 1 : 1) were synthesized through nucleophilic substitution ,hydrogenation and acidification. The nucleophilic substitution was reacted between 2-bromo-N-(2-nitrophenyl)acetam-ide and various substituted quinazolinone under the catalysis of NaH. Among them,2-bromo-N-(2-nitn>phenyl)acetamide was syn-thesized by a reaction between acetyl chloride and o-nitroaniline. And the substituted quinazolinone was synthesized by using amino-benzoic acid and formamide. The structures of these compounds were confirmed by 1H NMR, IR spectra and HRMS.