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 p...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.展开更多
文摘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.