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Pharmaceutical and Drug Development

Novel synthesis of protease inhibitors yield potent anti-HIV activity

Published in AIDS Weekly, June 7th, 2004

Novel synthesis of protease inhibitors yield potent anti-HIV activity.

"Novel indium-mediated radical cyclization reactions of aliphatic iodoalkynes have been studied. Treatment of iodoalkynes with a catalytic amount of In (0.1 equiv) and I-2 (0.05 equiv) promotes atom-transfer 5-exo cyclization to give five-membered alkenyl iodides," investigators writing in the Journal of Organic Chemistry report.

"In contrast," R. Yanada and colleagues reported, "reaction with In (2 equiv) and I-2 (1 equiv) yields reductive 5-exo cyclization products via the same 5-exo cyclization. Both processes are most likely initiated by low-valent indium...

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