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[Synthesis of hirsutrin and hyperin]

OBJECTIVE: To investigate an easier method for preparation of hirsutrin and hyperin. METHODS: Rutin was utilized as the starting material. The target compounds were produced via benzoylation, hydrolysis, glycosidation and deproteination. RESULTS: The yield of key intermediate 5,7,3',4'-tetra-O-benzoyl quercetin was improved by reducing the hydrolysis time of 5,7,3',4'-tetra-O-benzoyl rutin in HCl/EtOH. Hirsutrin and hyperin were synthesized. CONCLSION: Hirsutrin can be synthesized and the yield of hyperin improved by this method.