METHOD OF PREPARING RACEMIC TOTERODINE, INTERMEDIATE OF RACEMIC TOLTERODINE, AND METHOD OF PREPARING THE SAME

摘要

A method for manufacturing a tolterodine racemate, the intermediate of a tolterodine racemate, and a method for manufacturing the intermediate are provided to reduce the reaction time and to lower the manufacturing cost. A method for manufacturing a tolterodine racemate comprises the steps of reducing the ethyl benzoyl acetate of the formula 2 into the phenylpropane-1,3-diol of the formula 3; selectively sulfonating the primary hydroxyl group of the phenylpropane-1,3-diol of the formula 3 to produced the compound of the formula 4; directly substituting the compound of the formula 4 with diisopropylamine to produce the compound of the formula 5; and Friedel-Crafts alkylating the compound of the formula 5 in the presence of a catalyst to produce the tolterodine racemate of the formula 5.