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

• DOI: 10.1021/acs.orglett.6b00404
• Publication Date: 2016-03-07T16:09:41Z
• Authors: Atul A. More; Chepuri V. Ramana
• Keywords: Benzofuran; Integrase inhibitor

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