Synthesis And Antifungal Activity Of 3,3-dimethyl-1-(1H-1,2,4-triazole-1-yl)butan-2-One Derivatives

Triazole fungicide has drawn much attention because of its high efficiency,low toxicity,broad-spectrum of antifungal activity,low resistance,and the diversity of the chemical structure.It is still a hot research topic to develop new fungicide at present.3,3-dimethyl-l-(1H-1,2,4-triazol-l-yl)butan-2-one is an important intermediate to synthesize triazole fungicides,It has a variety of chemical reactivity such as reduction,epoxidation,oximation,alkylation,condensation,Wittig reaction and Michael addition,etc.In this paper,twenty compounds were designed and synthesized from 3,3-dimethyl-1-(1H-1,2,4-triazol-1-yl)butan-2-one by condensation and addition,The structures of all compounds were confirmed by means of 1H NMR,13C NMR and Ms,The antifungal activity of all compounds were determinedd against 6 plant pathogenic bacteria by mycelium growth rate method at the concentration of 50 mg/L.The preliminary bioassay showed that some compounds exhibited good antifungal activities,The inhibition rates of compound T6,T8,T11,T17 against Fusarium graminearum,T4,T6,T11 against Colletotrichum Gloeosporioiles,T4,T6,T8,T10,T11,T16,T17,T18,T20 against Cytospora Mandshurica,T4,T10,T17 against alternaria solani are above 90%.Compounds T4,T10,T17 have a greater inhibitory effect on alternaria solani than the positive control(86.27%)All of the compounds showed no obvious antifungcal activities against Curvularia lunata.boed and Pyricularia Grisea.The structure-activity relationships of these compounds indicated that a suitable substituent at the 1-position is impotant for the antifungal activity.