天然产物Thiasporine A及其类似物的合成与生物活性

Synthesis and Bioactivity of Thiasporine A and Its Analogues

[目的]首次对天然产物thiasporine A及其类似物的农用生物活性进行测试。[方法]以取代的苯甲腈和3-溴丙酮酸乙酯为原料,经多步反应合成了thiasporine A及其类似物,结构经过^(1)H NMR,^(13)C NMR和高分辨质谱分析确证。[结果]Thiasporine A及其类似物合成简单,具有较高的杀真菌活性,以及一定的杀虫、除草活性,可作为绿色、安全噻唑类新型杀菌剂创制的天然先导结构,值得进一步探索研究。

[Aims]This study aims to test the agricultural biological activity of thiasporine A and its analogues for the first time.[Methods]In this study,the substituted benzonitrile and ethyl 3-bromopyruvate were used as raw materials to synthesize thiasporine A and its analogues through a multi-step reaction.Their structures were confirmed by ^(1)H NMR,^(13)C NMR,and HRMS analysis.[Results]The research results showed that thiasporine A and its analogues are simple to synthesize,and exhibited strong fungicidal activities,certain insecticidal and herbicidal activities,which can be used as a natural lead structure for the creation of new green and safe thiazole fungicides,and are worthy of further exploration.