Enzymatic preparation of optically active fungicide intermediates in aqueous and in organic media

Abstract

Pure stereoisomers of two new triazole and morpholine fungicides were prepared starting from enzymatically synthesized chiral alcohols intermediates. Two resolution strategies were compared: lipase-catalyzed hydrolysis of corresponding acetates in water and lipase-catalyzed transestérification of alcohols in organic solvent. The antifungal activity of optically pure enantiomers of the synthesized fungicides were investigated In vitro and in vivo against a variety of fungi, showing an activity ratio (R-form / S-form) up to 400. © 1992, Walter de Gruyter. All rights reserved.