A series of novel 1-substituted phenyl or glycosyl 1,2,3-triazoles was designed and synthesized by azide-alkyne 1,3-dipolar cyeloaddition between 4,6-dimethoxy-2-[（4-prop-2-ynyl）piperazin-l-yl]pyrimidine and each of...A series of novel 1-substituted phenyl or glycosyl 1,2,3-triazoles was designed and synthesized by azide-alkyne 1,3-dipolar cyeloaddition between 4,6-dimethoxy-2-[（4-prop-2-ynyl）piperazin-l-yl]pyrimidine and each of different azides catalysed by in situ generated Cu（I）. The O-acyl protecting groups on glycosyl 1,2,3-triazoles were removed by triethylamine in wet methanol. Their chemical structures were established on the basis of corresponding tH NMR, 13C NMR, MS and elemental analysis. The fungicidal activities of target compounds were evaluated in vitro against Fusarium omysporum, Physalospora piricola, Alternaria solani, Phytophthora capsici, Cercospora arachi- dicola and Gibberella zeae at 50 μg/mL. The bioassay results indicate that some of the compounds exhibited mode- rate but promising fungicidal activities. In particular, acetylated glucopyranosyl triazole displayed a good fungicidal activity against Physalospora piricola, which is equal to that of the positive control compound chlorothalonil.展开更多
基金Supported by the National Basic Research Program of China（No.2010CB126106）, the Fundamental Research Funds for the Central Universities and Natural Science Foundation of China（No.31000861）.
文摘A series of novel 1-substituted phenyl or glycosyl 1,2,3-triazoles was designed and synthesized by azide-alkyne 1,3-dipolar cyeloaddition between 4,6-dimethoxy-2-[（4-prop-2-ynyl）piperazin-l-yl]pyrimidine and each of different azides catalysed by in situ generated Cu（I）. The O-acyl protecting groups on glycosyl 1,2,3-triazoles were removed by triethylamine in wet methanol. Their chemical structures were established on the basis of corresponding tH NMR, 13C NMR, MS and elemental analysis. The fungicidal activities of target compounds were evaluated in vitro against Fusarium omysporum, Physalospora piricola, Alternaria solani, Phytophthora capsici, Cercospora arachi- dicola and Gibberella zeae at 50 μg/mL. The bioassay results indicate that some of the compounds exhibited mode- rate but promising fungicidal activities. In particular, acetylated glucopyranosyl triazole displayed a good fungicidal activity against Physalospora piricola, which is equal to that of the positive control compound chlorothalonil.
