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Updated: Apr 18, 2026

Rapid Screening of HIV Reverse Transcriptase and Integrase Inhibitors
Published on: April 9, 2014
An efficient and highly diastereoselective synthesis of GSK1265744, a potent HIV integrase inhibitor
Huan Wang1, Matthew D Kowalski, Ami S Lakdawala
1Global API Chemistry, ‡MDR Chemical Science, §Analytical Sciences, GlaxoSmithKline , 709 Swedeland Road, King of Prussia, Pennsylvania 19406, United States.
Abstract:
A novel synthesis of GSK1265744, a potent HIV integrase inhibitor, is described. The synthesis is highlighted by an efficient construction of the densely functionalized pyridinone core as well as a highly diastereoselective formation of the acyl oxazolidine moiety. The latter exploits the target molecule's ability to chelate to Mg(2+), a key feature in the integrase inhibitor's mechanism of action.
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