NEW MATERIAL:An optically active 2-hydroxy-2-(substituted phenyl)ethylthiourea derivative expressed by formula I (R is lower alkyl).
EXAMPLE: (+)-N-[2-Hydroxy-2-(chlorophenyl)ethyl]-N'-(methyl)thiourea.
USE: A medicine, having excellent antiulcer action and useful for preventing and treating ulcer in digestive tracts.
PREPARATION: The racemic modification of a compound expressed by formula II is resolved as diastereomers using a natural optically active organic acid, e.g., D-tartaric acid, to provide optically active amino-alcohols expressed by formula II, which are then reacted with an isothiocyanate expressed by the formula RNCS in a solvent, such as acetonitrile, at a temperature of 0°C to the boiling point of the solvent for 30min-3hr to afford the optically active compound expressed by formula I.
KOJIMA KOJI
HIKITA JUTARO
OKUMA HARUO