2-取代的6-溴甲基-4(3H)-喹唑啉酮的合成  

Syntheses of 2-Substituted 6-Bromomethyl 4(3H)-Quinazolinones

作　　者：曹胜利[1] 冯玉萍[2] 高红核[1] 冯克然[1] 

机构地区：[1]首都师范大学化学系,北京100037 [2]清华大学化学系,教育部生命有机磷化学与化学生物学重点实验室

出　　处：《应用化学》2005年第9期1027-1029,共3页Chinese Journal of Applied Chemistry

基　　金：北京市自然科学基金资助项目(7002006;7042006);教育部科学技术研究重点项目(2002KJ091)

摘　　要：2-Amino-5-methylbenzoic acid（1） was acylated with acyl chlorides,then heated（together） with（acetic） anhydride to give 2-phenyl or 2-benzyl-6-methylbenzoxazin-4-one（3a3b）,while compound 1 was （reacted） with propanoic anhydride or trifluoroacetic anhydride to give 2-ethyl or 2-trifluoromethyl-6-methylbenzoxazin-4-one（3c3d） directly. Then,2-substituted 6-methylbenzoxazin-4-ones（3a3d） were heated together with formamide to afford 2-substituted 6-methyl-4（3H）-quinazolinones（4a4d）,which were（converted） into the title compounds（5a5d） via brominating with N-bromosuccinimide in the presence of （PhCOO）2.The structures of all the intermediates and final products were confirmed with ESI-MS,1H NMR and elemental analysis.2-Amino-5-methylbenzoic acid （1） was acylated with acyl chlorides, then heated together with acetic anhydride to give 2-phenyl or 2-benzyl-6-methylbenzoxazin-4-one （3a - 3b）, while compound 1 was reacted with propanoic anhydride or trifluoroacetic anhydride to give 2-ethyl or 2-trifluoromethyl-6-methylbenzoxazin-4-one （3c - 3d） directly. Then, 2-substituted 6-methylbenzoxazin-4-ones （ 3a - 3d ） were heated together with formamide to afford 2-substituted 6-methyl-4 （3H） -quinazolinones （ 4a - 4d ）, which were converted into the title compounds （Sa - 5d） via brominating with N-bromosuccinimide in the presence of （PhCOO） 2. The structures of all the intermediates and final products were confirmed with ESI-MS, ^1H NMR and elemental analysis.

关 键 词：4(3H)-喹唑啉酮 苯并噁嗪酮 N-溴代琥珀酰亚胺 合成 

分 类 号：O621.3[理学—有机化学]