NEW MATERIAL:L-Lysine salt of d-threo-2-hydroxyl-3-(2-aminophenylthio)-3-(4- methoxyphenyl-)-propionic acid of formula I (*C means the carbon of the molecule which has been optically resolved).
USE: A synthetic intermediate of medicines. It is used as a synthetic intermediate of diltiazem hydrochloride, a remedy for angina pectoris and essential hypertension.
PREPARATION: dl-threo-2-Hydroxyl-3-(2-aminophenylthio )3-( 4-methoxyphenyl )-propionic acid of formula II and L-lysine or a salt of the propionic acid and L-lysine salt are allowed to react in a solvent such as methanol whereby the corresponding salt is obtained. Two kinds of the optically active diastereomers formed are separated by utilizing the difference in solubility between them and the compound of formula I is obtained as a hard soluble component.
ISHIZUKA YORIYASU
FUTSUKAICHI OSAMU
SANYO KAGAKU KENKYUSHO KK
US4533748A | 1985-08-06 |