Total Synthesis of Integrastatin B Enabled by a Benzofuran Oxidative Dearomatization Cascade

The first total synthesis of integrastatin B, a potent HIV-1 integrase inhibitor, has been accomplished in seven steps with a 17.9% overall yield employing easily accessible starting compounds. The Oxone-mediated oxidative benzofuran dearomatization cascade has been employed as the key skeletal construct to forge the central tetracyclic nucleus.

强效HIV-1整合酶抑制剂整合他汀B（integrastatin B）的首例全合成已成功实现：以易于获取的起始原料为底物，通过7步反应即可完成，总收率达17.9%。本研究采用Oxone介导的氧化苯并呋喃脱芳构化级联反应作为关键骨架构建策略，成功构筑了该分子的中心四环骨架。