Enantio-conversion and -selectivity of racemic atenolol kinetic resolution using free Pseudomonas fluorescens lipase (Amano) conducted via transesterification reaction

Abstract

In this report, effects of reaction parameters on kinetic resolution of racemic atenolol using Pseudomonas fluorescens lipase were investigated via transesterification for production of pharmacologically active eutomer (S)-atenolol with high enantiomeric purity. It was found that a temperature of 45 °C produced an acceptable enantioselectivity (E: 17). Good agitation speeds were found at 170–230 rpm producing E values of 12–15, whilst an enzyme activity of ≥2500 U gave 100% conversion of the (S)-atenolol. Substrate concentrations of 11.26–18.80 mM gave E values of 11.6–12.3. Variation of the substrate molar ratio yielded (S)-atenolol conversions of 44.67–61.58% with E = 12–23.