Design, Synthesis And Fungicidal Activities Of Strobilurin Analogues By Click Chemistry

Recent advances on the development of Triazole and strobilurins derivatives display a wide range of fungicidal activities, and have been widely used as fungicides. In order to find novel lead compounds of fungicidal activities.38 novel strobilurin analogues containing 3,4-dihydropyrimidin-2(1H)-one and pyrimidine moieties were designed and synthesized by click chemistry according to the principles of combination of bioactive groups and bioisosterism. Their structures were comfirmed by 1H NMR and elemental analysis, some of them were further determined by IR and MS. Their structures are listed as follows:(1)Strobilurin analogues containing 3,4-dihydropyrimidin-2(1H)-one side chain Ia～Ik; (2)Strobilurin analogues containing pyrimidine moieties side chain Ⅱa-Ⅱi; (3)Strobilurin oxime ether analogues containing pyrimidine compound side chain Ⅲa1-Ⅲi2;Their preliminary fungicidal activities of all target compounds were evaluated. The bioassays indicated that some of the target compounds exhibited good fungicidal activities. Their structures and fungicidal activities relationships are also studied.