PRODUCTION OF OPTICALLY ACTIVE (S)-(+)-3-(2,3-EPOXYPROPOXY)-4-MORPHOLINO-1,2,5-THIADIAZOLE

摘要

PURPOSE:To obtain the title compound useful as a synthetic intermediate for beta-adrenergic nerve blocker by subjecting hydroxymorpholinothiadiazole and [R]-glycodol to oxidation-reduction condensation through dehydration in the presence of triphenylphosphine, etc. CONSTITUTION:3-Hydroxy-4-morpholino-1,2,5-thiadiozole shown by formula I and [R]-glycodol shown by formula II are subjected to oxidation-reduction condensation through dehydration in an inert organic solvent (e.g. ether, THF or benzene) in the presence of triphenylphosphine or dialkylazodicarboxylic acid ester (e.g. diethylazodicarboxylic acid ester) to give the aimed compound shown by formula III.