Design, synthesis and agricultural evaluation of derivatives of N-Acyl-N-(m-fluoro-benzyl)-6-amino-coumarin.

ABTRACTThis study aims to design and synthesize a series of N-Acyl-N-(m-fluoro- benzyl)-6- amino-coumarins through the principle of active substructure stitching, which are based on the core structure of N-(m-fluoro-benzyl)-6-amino-coumarin. The structures of target compounds have been characterized by H NMR, C NMR, ESI-MS and elemental analysis. Meanwhile, their agricultural activity have been evaluated in two weeds ( and ) and four widespread noxious pathogens ( and ). The herbicidal activity results showed that almost all synthetic molecules have a greater impact on the stem system than on the root. Excellent inhibition rates were discovered from compounds and against on stems, which were above 58%(20 mg/L), 68%(100 mg/L) respectively. Compounds and also exhibited striking inhibition on stems growth of both weeds. Anti-pathogenic activity showed that all the compounds exerted a better inhibitory activity on at 20 ppm compared to control carbendazim. All the heterocyclic substituted compounds (, >57%) made a better influence than the control (54.1%) at the100 ppm. This research provides promising herbicidal and anti-pathogenic agents that have the better effects and can be potential for further development.