Synthesis of enantiomerically pure 4-aryl-3,4-dihydro-pyrimidin-2(1H)-ones via enzymatic resolution:: preparation of the antihypertensive agent (R)-SQ 32926

A practical and short synthesis of the enantiomerically pure dihydropyrimidone antitypertensive agent (R)-SQ 32926 has been developed. The key step in the synthesis is the enzymatic resolution of an N3-acetoxymethyl-activated dihdropyrimidone precursor by Thermomyces lanuginosus lipase. The absolute configuration of (R)-SQ 32926 was confirmed by circular dichroism spectroscopy. (C) Elsevier Science Ltd. All rights reserved.