吡啶衍生物研究(Ⅺ):2-仲丁胺基-5-(2-氯吡啶-4-基)-1,3,4-噻二唑对映异构体的合成及除草活性

Studies on Pyridine Derivatives (Ⅺ):Synthesis and Herbicidal Activities of Both Enantiomers of2-sec-Butylamino-5--1,3,4-thiodiazoles

摘要: 2-仲丁胺基-5-(2-氯吡啶-4-基)-1,3,4-噻二唑(BCPT)是早期发现的一个具有良好除草活性的外消旋先导化合物,报道了使用R/S-仲丁胺为原料分别合成BCPT的两个对映异构体的方法。初步生测结果显示,3种噻二唑化合物(外消旋体和两个对映异构体)对稗草的根和茎均表现出较强的抑制作用,其中S-(+)对映异构体对茎的抑制作用强于R-(-)对映异构体和外消旋体,但对根的生长抑制作用三者间没有显著差异。

Abstract: Both enantiomers of 2-sec-butylamino-5-(2-chloropyrid-4-yl)-1,3,4-thiodiazoles (BCPT),a powerful racemic herbicidal compound which was found in previous research,were synthesized from R- and S-butylamine respectively.The preliminary bioassay results showed that three of the thiodiazoles (racemate and enantiomers) were excellent growth inhibitors to both roots and stems of barnyard grass.The S-(+) enantiomer was the strongest for stem growth inhibition,and R-(-) enantiomer was the weakest.But they had little inhibiting difference on root growth.