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

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posted on 07.03.2016, 16:07 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.