The benzofuranyl motif present in compounds exhibits various medicinal properties and non-drug applications. These derivatives are naturally occurring compounds or synthetic materials, which cover a broad spectrum of pharmacological activities like anti-inflammatory, anti-diabetic, anti- depressant, anti-HIV, anti-microbial, anti-proliferative, anti-convulsant, cytotoxic, analgesic, etc. Few of the commercially interesting compounds from this class are, ailanthoidol (anti-inflammatory), amiodarone, dronedarone, celivarone (anti-arrhythmic), bufuralol (muscular airways relaxant), morphine, 5-(2-aminopropyl)benzofuran; 5-APB, 6-(2-aminopropyl)benzofuran; 6-APB (CNS), rifampicin (antibiotic), etc., whereas, some of the non-drug applications are in perfumery industry (bergapten) and as tannin activators in sunscreen preparations (psoralen, 8-methoxypsoralen, and angelicin). Considering these interesting biological activities and commercial utilities, a review on the synthetic aspects of this privileged scaffold was attempted. For the benefit of natural product-based drug discovery, available sources of these derivatives, extraction process and reported biological activities have also been outlined in this review.

化合物中存在的苯并呋喃基基序具有多种药用特性和非药物应用。这些衍生物是天然存在的化合物或合成材料，涵盖了广泛的药理活性，例如抗炎，抗糖尿病，抗抑郁，抗HIV，抗微生物，抗增殖，抗惊厥，细胞毒性，止痛药这类中很少有商业上令人感兴趣的化合物是艾蒽环醇（抗炎药），胺碘酮，决奈达隆，西维酮（抗心律不齐），布法洛尔（肌肉气道松弛剂），吗啡，5-（2-氨基丙基）苯并呋喃；等等。5-APB，6-（2-氨基丙基）苯并呋喃; 6-APB（CNS），利福平（抗生素）等，而某些非药物用途则用于香水业（bergapten），并用作防晒制剂中的单宁激活剂（补骨脂素，8-甲氧基补骨脂素和当归）。考虑到这些有趣的生物学活动和商业用途，试图对该特权支架的合成方面进行综述。为了有利于基于天然产物的药物发现，本综述还概述了这些衍生物的可用来源，提取过程和报道的生物活性。