Variations in the phytochemical composition and antioxidant properties were studied in the wine of wampee leaves obtained at different stages of fermentation process. The highest concentrations of total phenolic and flavonoid contents were attained at Day 12 and Day 21 of fermentation, respectively. In addition, five phytochemical compounds including vanillic acid, p ‐coumaric acid, rutin, ferulic acid, and 7‐hydroxycoumarin were identified and quantified by HPLC in fermented wampee products. The strongest antioxidant activity in wine was monitored on Day 12. Furthermore, total antioxidant activity was significantly correlated with vanillic acid, p ‐coumaric acid, ferulic acid, and 7‐hydroxycoumarin compared with rutin. The obtained results suggested that 12‐day fermentation could be an optimal process for excavation of applying wampee leaves into food and wine industries.