METHOD FOR THE PREPARATION OF (R)-TOLTERODINE TARTRATE

摘要

The invention relates to a method for the preparation of (R)-tolterodine tartrate, comprising the following steps in which: a benzopyranone having formula 1 is reduced with sodium borohydride in order to form a dialcohol having formula 12; the hydroxyl groups of the dialcohol are reacted with mesyl chloride in order to introduce two methanesulphonyl groups and to form a dimesylated compound having formula 13; the dimesylated compound is reacted with diisopropylamine under pressure and, subsequently, with sodium hydroxide in order to obtain tolterodine which is isolated in the form of the corresponding hydrobromide having formula 14; the base tolterodine is released from the hydrobromide; and the tolterodine is reacted with (+)-tartaric acid in order to prepare the (R)-tolterodine tartrate.