Chemical synthesis study demonstrates a scalable asymmetric route to the anti-HIV agent MK-8527, highlighting efficient kilogram-scale production with high purity.
A practical and asymmetric synthesis of potent anti-HIV nucleoside MK-8527 is described. The key discoveries are a novel stereoselective dynamic kinetic resolution (DKR) Mitsunobu glycosylation and selective amination of the resulting 2,6-dichloro nucleoside. The new route was successfully demonstrated on the kilogram scale and provided isolated MK-8527 with more than 99% HPLC purity through crystallization.
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Whittaker et al. (2026) studied this question.
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