Toward the Cure

The article illustrated outlines a highly efficient four-step synthesis method for a key intermediate in the production of the anti-HIV drug lenacapavir. Led by Juan C. Caravez and his team, the research details a novel approach, featuring a 1,2-addition to an aldehyde using an organozinc halide derived from a commercially available difluorobenzyl Grignard reagent. The process includes the oxidation of the resulting secondary alcohol using catalytic amounts of TEMPO with NaClO as a terminal oxidant, achieving an impressive 67% overall yield. The synthesis holds significant potential for cost-effective large-scale production of lenacapavir, addressing accessibility concerns, especially in low and middle-income regions.
More here: https://doi.org/10.26434/chemrxiv-2023-wls6x