A series of new pyrazolopyrimidine derivatives containing sulfur atom 5 has been designed and synthesized by treatment of carbodiimide 3, which came from iminophosphorane 2 undergoing a aza-Wittig reaction with phenyl ioscyanate, with alkylamine. The structures of compounds 5 were confirmed by 1H NMR, IR, EI-mass spectroscopy, and elemental analysis. The results of preliminary bioassay indicate that most compounds 5 exhibit an inhibition effect against Cercospora beticola, Botryosphaeria berengeriana, and Pellicularia sasakii, and compound 5g s...