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以取代2-氨基苯甲酸(1)为原料,经系列反应合成关键中间体β-乙氧酰基膦亚胺(4),再与芳基异氰酸酯、乙醇胺进行三组份串联的氮杂-Wittig反应,合成了一系列2-芳氨基-3-羟乙基-4(3H)-喹唑啉酮衍生物6.目标分子的结构通过IR,1H NMR,MS和元素分析确证,并进一步测试了目标化合物对烟草青枯菌的室内抑菌活性.结果表明,虽然所有化合物的抗菌活性抑制率均低于参照药物噻菌铜,但若喹唑啉酮母环附加有取代基时,化合物的抑菌活性得到显著的提高.由此可见,对喹唑啉酮母环进行修饰也不乏是一种改进其生物活性的有效途径.
The key intermediate β-ethoxycarbonylphosphinimine (4) was synthesized by a series of reactions using 2-aminobenzoic acid (1) as the starting material, and then reacted with aryl isocyanate and ethanolamine in a three-component aza-Wittig reaction , A series of derivatives of 2-arylamino-3-hydroxyethyl-4 (3H) -quinazolinone were synthesized. The structure of the target molecule was confirmed by IR, 1H NMR, MS and elemental analysis and the target The results showed that although the inhibitory rates of antibacterial activity of all the compounds were lower than that of the reference drug thiabendazole, when the quinazolinone ring was added with substituents, the antibacterial activities of the compounds Activity was significantly improved.Thus, the quinazolinone mother ring modification is also no lack of an effective way to improve its biological activity.