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

2016-03-07T16:07:42Z (GMT) by Atul A. More Chepuri V. Ramana
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.