Synthetic Study On Tolterodine Tartarate

Tolterodine tartrate is the improvement of competitive poison tain alkali receptor (M receptor antagonist,) is a kind of good efficacy treatment of unstable or overactive bladder infection drugs. It is the most widely used of bladder excessive activity of symptoms. However, China is currently an ageing society, with the increasing number of elderly patients with bladder excessive activity symptoms. These symptoms will reach a great number and also will produce great social benefits and economic benefits when studying the Tolterodine tartrate. Based on the domestic and foreign literatures, and on the basis of the reports of synthetic route analysis and comparison, Tolterodine tartrate was synthesized through the cyclization, methylation, reduction, sulfonylation, amidation,demethylation, separation from the starting material Cinnamic acid and P-cresp, and the process of Tolterodine tartrate's synthesis was studied and optimized. The process includes improving the important intermediates 4-6-methyl phenylsilicone-3-2-1-2H hydrogen--bta pyranoid ketone-2 and N, N-2-3-isopropyl (2-the-5-methyl phenylsilicone)-3-phenylmalonates amine synthesis'process and optimized separation process. Fumbling Through continuous learning and improvement, tartaric acid synthesis'process of the Tolterodine tartrate having better stability, simple operation, easy and cheap raw materials, high yield, high security, synthetic yield reached 25.6%(literature yield 17%), what's more, the process has been successfully completed in production, the fee of production is try to drop substantially, fully meet the requirements of industrial production.