Synthesisand Fungicidalactivityof1H-Pyrazole-4-Carboxamides

There are signs that pyrazole carboxamide derivatives activity may belower than1ppm, and has a new novel mechanism of action. According toour statistics on all new major abord pesticide companies patents, thesecompounds are focus of the research of the large foreign companies. I referto pyrazole carboxamide patents of syngenta in the year of2009. Retainactivity structure of N-methyl-3-difluoromethyl-4-pyrazole carboxamide,extend the bridge bond between the pyrazole ring and the benzene ring.Modified the benzene ring.The121novel difluoromethyl substituted pyrazole benzamidederivatives were synthesized with nucleophilic substitution, cyclization,hydrolysis, esterification and addition reaction using ethyl4,4–difluoro-3-oxobutanoate and triethoxymethane as raw materials.Their structures wereclearly confirmed by1H NMR and MS spectry. The antifungal activity test showed that target compounds ZJ19、ZJ56、ZJ57、ZJ66、ZJ72、ZJ104、ZJ107、ZJ108、ZJ110exhibit someinhiting effects against gibberella zeae、botrytis cinerea and rhizoctoniasolani at the50mg/L,similarly to the control(Compound1.197). They havegreat potential commercial value and worthy of further study.