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 2 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.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.化合物的合成具有合成路线短、产率高、原料易得等优点.目标化合物的结构均经1H NMR,IR 和 HRMS 等方法确证.
Tow novels N-(2-aminophenyl)-2-quinazolinone-acetamide hydrochloride were synthesized through nucleophilic substitution,hydrogenation and acidification.The nucleophilic substitution was reacted between 2-bromo-N-(2-nitrophenyl)acetamide and various substituted quinazolinone under the catalysis of NaH.Among them,2-bromo-N-(2-nitrophenyl)acetamide was synthesized by a reaction between acetyl chloride and o-nitroaniline.And the substituted quinazolinone was synthesized by using aminobenzoic acid and formamide.The new process is characterized by short synthetic route,high yield and cheap raw materials.The structures of these compounds were confirmed by 1H NMR,IR spectra and HRMS.