PROCESS FOR PREPARING TOLTERODINE AND THE L-TARTRATE THEREOF

摘要

The present invention relates to a process for preparing tolterodine and the L-tartrate thereof. The preparation consists of the following steps: A) ammonolysis reaction between diisopropylamine and compound 2 (3,4-dihydro-6-methyl-4-phenyl-2H-benzopyran-2-one) activated by an activator to afford the amide 3; B) reduction of the amide by a reductant to give compound 1, i.e., racemic tolterodine free base; C) Resolution of the tolterodine free base to afford tolterodine L-tartrate. The present route is very short and suitable for industrial production.