新型双嘧啶酮二苯醚的合成

以自制的4,4'-双甲酰基二苯醚类化合物、β-酮酸酯及脲为原料,在Fe C13·6H2O的催化下,通过Biginelli反应合成了12种新型双嘧啶酮二苯醚类衍生物(6a~6l),探讨了双嘧啶酮合成的反应历程并对反应条件进行优化.另外,对4,4'-双甲酰基二苯醚类化合物的合成方法进行了改进,通过控制对氟苯甲醛的加入时间,提高了产率,并大大缩短了反应时间.对所有化合物进行了室内毒力测试,结果表明,化合物6d,6h和6i的抗菌效果较好,对西瓜枯萎病的EC95值均小于对照药三唑酮;当取代基R2为CF3时,化合物的杀菌抑菌活性较好.

Synthesis of Novel Dipyrimidinone Diphenyl Ethers

Generally, many diphenyl ethers show good bioactivity, the advances of these kind of compounds in medical area have made the synthesis research becoming a hot topic. In this work, through the Biginelli''s condensation of 4,4''-diformyl diphenylethers, β-ketoesters and urea catalyzed by FeC13·6H2O, 12 novel dipyrimidinone diphenyl ethers were synthesized. The synthesis mechanism of dipyrimidinone was discussed and the reaction conditions were optimized. In the meantime, the synthetic method of 4,4''-diformyl diphenyl ether derivatives was also improved. Due to the appropriate timing of the reactants and catalyst''s addition, this method had the advantage of short reaction time and excellent yields(90%). Finally, the preliminary toxicity testing of all the target compounds was investigated.The results showed that EC95 of compounds 6d, 6h and 6i were smaller than the comparison compound to Fusarium oxysporium f.s.p. niveum. The compounds containing R2 (CF3) had better biological acitivity than the others.