Synthetic study demonstrates stereoretentive esterification of carboxylic acids with phenols, indicating a sustainable route for late-stage drug functionalization.
A green, stereoretentive esterification of carboxylic acids with phenols has been developed using N‐methylimidazole (NMI) as the catalyst and pivalic anhydride (Piv 2 O) as the carboxylic acid activator. The reaction proceeds in ethyl acetate, exhibits broad functional group tolerance and minimal racemization, and generates pivalic acid as a readily separable byproduct. This mild, atom‐economical strategy enables late‐stage functionalization of pharmaceutical molecules, providing a sustainable route toward phenolic esters.
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Qi et al. (2026) studied this question.
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