Clemastine is an effective antihistamine drug having sedative and anticholinergic effects. The main substrate for manufacturing of clemastine is (R)-2-(1-mehyl-2-pyrrolidine)ethanol, which can be also an important chiral building block for the synthesis of biologically active compounds. Starting from the racemic 2-(1-methyl- 2-pyrrolidine)ethanol as a substrate, an enzymatic procedure was developed for the efficient synthesis of corresponding highly enantiomerically enriched (R) and (S)-2-(1-methyl-2-pyrrolidine)ethanol. Various commercially available immobilized and not immobilized lipases were examined and several acyl donors, as a acylating agents in enzymatic kinetic resolution were applied. Some parameters of enzymatic reactions, as temperature, solvent, time and substrates ratio were optimized. Spectroanalysis data, enantiomer excess, specyfic rotation and other physical parameters of obtained compounds were determined.

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