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This review summarizes the synthetic methods, reaction and biological application of benzofuran derivatives during the period from 1990 to 2021. This review a broad view of chemistry of benzofuran derivatives and it includes the literature survey on methods of preparations, reactions and pharmacological activities in these derivatives. The benzofuran ring is a common structure element that appears in a large number of medicinally important compounds. The benzofuran nucleus is widely distributed in natural products particularly among plant Kingdom.