Abstract

AbstractAn efficient kinetic resolution of a variety of racemic 2‐hydroxyarylketone derivatives was developed by asymmetric esterification protocol using diphenylacetic acid, pivalic anhydride, and a catalytic amount of (R)‐benzotetramisole ((R)‐BTM). It was revealed that employing a tertiary amine as a co‐base in this reaction is not necessary to achieve high s‐values. All conducted reactions proceeded smoothly with good s‐values under the optimized reaction conditions, irrespective of the steric and electronic nature of the substituents on the aromatic rings of the substrates. The most stable transition state of the reaction was determined by density functional theory (DFT) calculations.

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