Abstract:Using 2-hydroxy-5-nitrobenzaldehyde as starting compound, ten novel 8-aminobenzo[4,5]furo [3, 2-d]pyrimidine derivatives were synthesized through cyanation, esterification, cyclization and chlorization. Title compounds were fully characterized by 1H NMR, 13C NMR, IR, and MS. In addition, the reaction conditions were explored, and got optimized condition.