A concise asymmetric synthesis of triazole antifungal agent voriconazole is described. Salient features of this synthesis include a LiOH‐controlled highly stereospecific formation of ( Z )‐enol triflate from 2‐difluorobenzene acetoacetate to access the crucial tetrasubstituted ( Z )‐allylic alcohol, and a highly enantioselective VO(O i Pr) 3 /BHA ligand‐catalyzed epoxidation to construct the critical contiguous carbon stereocenters in a single step.
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Peng et al. (2024) studied this question.
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