Eight novel 5,7-disubstituted-2-{5-methyl-3-（4-trifluoromethylphenyl）isoxazol-4-ylcarbonylimino}-2H-1,2,4-thiadiazolo[2,3- a]pyrimidines were synthesized by multi-step reactions in yields 68-85%.Reactions were carried out either by ultrasound irradiation or conventional method,and found it was faster and more efficient under ultrasonic irradiation.Preliminary herbicidal activities against Echinochloa crus-galli,Digitaria sanguinalis and Chenopodium serotinum were also evaluated by flat-utensil method,and the results indicated that the target compounds exhibited significant activities,some were even higher than the control herbicide.
Mao Rong WangLin JiangShao Fang ZhouZe Yuan ZhangZeng Chen Ji
Twelve novel compounds of 2-acetyl-lH-benzimidazole oxime-ethers and 2-acetyl-6-chloro-1H-benzimidazole oxime-ethers were synthesized with o-phenylenediamine （or 4-chloro-o-phenylenediamine）, 2-hydroxypropyl acid, alkoxy （or benzyloxy） amines hydrochloride as starting materials. The structures of the target compounds were characterized by IR, 1H NMR spectra and elemental analyses. The in vitro fungicidal activities against Botrytis cinerea Pers and Alternaria alternata were also evaluated by mycelium growth rate method. The results indicate that the compounds 3b, 3c, 3f, 3g and 3h exhibit good activities against Botrytis cinerea Pers, while 3b and 3f possess excellent activities against Alternaria alternate, and their fungicidal activities are all higher than that of carbendazim.
A series of novel 1H-benzimidazol-1-yl acetates and 1H-benzimidazol-1-yl propionates containing 1H-1,2,4-triazole moiety were synthesized under microwave irradiation by multi-step reactions, in yields of 87-94%. Their in vitro antifungal activities against Botrytis cinerea and Sclerotinia sclerotiorum were evaluated by mycelial growth rate method. All the target compounds exhibit high activities against B. cinerea with the EC50 values of 7.96-21.74 μg/mL, higher than that of carbendazim.
