PROCESS FOR THE OPTICAL RESOLUTION OF RACEMIC MIXTURES OF ALPHA-NAPHTHYL PROPIONIC ACID

摘要

Optical resolution of racemix mixts. of alpha-naphthylpropionic acids of formula (I) comprises: (A) reacting a racemic mixt. of a cpd. of formula (II) with an optically active substance of formula R4-NH2, to obtain a pair of diastereoisomeric amides; (B) heating, dissolving and cooling the pair of diastereoisomeric amides to be resolved into the single diastereoisomers; and (C) acid hydrolysing the obtd. single diastereoisomeric amide to obtain the desired optically active alpha-naphthyl-propionic acid of formula (III). In the formulas, R1=Me; R2=H or halogen; R3= halogen, C1-2 alkoxy or C5 alkoxy substd. by halogne; R4= R5CHCH2OH or R6C(OH)HCH2, which form active beta- amino alcohol by binding with -NH2(R5 and R6 are C1-6 alkyl).