| 摘要 |
NEW MATERIAL:The salt of the propionic acid derivative of formula I (Ar is lower alkoxy-substituted phenyl) and alpha-phenylethylamine. USE:A synthetic intermediate of pharmaceuticals. For example, it is useful as a synthetic intermediate of a vasodilator, diltiazem hydrochloride. PREPARATION:The compound of formula I (threo-type) is prepared by reacting 2-aminothiophenol with the glycidic acid ester of formula II (R<3> is eater residue) in a solvent at 100-140 deg.C, and hydrolyzing the reaction product. The optical resolution of the propionic acid derivative can be carried out reacting the racernic compound of the propionic acid derivative of formula I with an optically active alpha-phenylethylamine to obtain the corresponding salt, and separeting and collecting the produced hardly soluble salt and the easily soluble salt from each other taking advantage of the solubility difference of the optically active salts.
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