关键词: 喹唑啉-4（3H）-酮, 氮杂-Wittig反应, 合成, 杀菌活性

Key intermediate β-ethoxycarbonyl iminophosphorance (4), which was prepared from starting material substituted 2-aminobenzoic acid (1), was reacted with aryl isocyanates, ethanolamine by a three-component tandem aza-Wittig reaction to obtain a series of 2-arylamino-3-hydroxyethyl-4(3H)-quinazolinone derivatives 6. The structures of the target products were confirmed by IR, ¹H NMR, MS and elemental analysis. The antibacterial activities of compounds 6 in vitro against tobacco bacterial wilt were further tested. The bioassay of the compounds 6 showed that the inhibitory activities of all the compounds were lower than the reference drug thiediazole copper. However, the antibacterial activity was significantly enhanced when the parent quinazolinone rings of the compounds 6 are substituted. Thus it can be seen that decoration of the parent quinazolinone ring of the compounds 6 can be regard as a kind of effective way of improving their biological property.

Key words: quinazolin-4(3H)-one, aza-Wittig reaction, synthesis, bactericidal activity