Synthesis of substituted novel quinazolinone compounds / 药学实践杂志

ABSTRACT

Objective To optimize the synthesis route of substituted quinazolinone and investigate the influence of tem-perature and time in the synthesis of key intermediates .Methods A parallel test was carried out to compare temperature ,time and the ester bond ammonolysis of condensing agent ,including the total analysis of experimental result .And orthogonal experi-mental design was used and the influence of temperature and time on the yield were investigated .Results and Conclusion The structure of the compound was confirmed by 1 H NMR ,MS and 13C NMR .When the reaction temperature was 30 ℃ ,the reac-tion time was 24 h with the condensing agent (DCC) and the reactant ratio of 1 .5∶1 ,the yield of ester bond ammonolysis was higher .The optimal preparation procedure of quinazolinone compounds was more available for industrial production .In vitro antifungal activity test results showed that the lead compounds measured on five clinical pathogenic fungi have the potential an-tifungal activity ,and are worth for further study .