METHOD FOR PREPARING OF R- (+)- 1- METHYL- 2- (HYDROXYETHYL)- PYROLIDENE

The method is intended for application in the pharmaceutical industry and the compound obtained thereby is used in the manufacturing of 2-(2-(p-chloro-)-α-methyl-α-phenyl/benzyl/oxi/ethyl-1-methylpyrolidene hydrogenfumarate, the active ingredient of an antihistamine agent. The R-(+)-1-methyl-2-(2-hydroxyethyl)-pyrolidene is prepared by a simplified method, without separation of the intermediate products, at high yield and is of high optical purity. N-methyl-2-pyrolidinethione is alkylated with benzylbromoacetate, the resulting salt is treated with triphenylphosphine and triethylamine, the 2-(benzyloxicarbonyl methylidene)-1-methylpyrolidine thus obtained is reduced by sodium cyanoborohydride to an N-methyl-2-(2-pyrolidinyl) acetic acid benzyl ester racemate. The ester is subjected to racemic resolution using (+)-di-p-toluyl-tartaric acid to give the optically active benzyl ester of the N-methyl-2-(2-pyrolidinyl) acetic acid, which is then reduced with lithium aluminium hydride.