A new efficient route to tolterodine

…, T Corrias, M Marchetti, S Paganelli…

Index: Botteghi, Carlo; Corrias, Tatiana; Marchetti, Mauro; Paganelli, Stefano; Piccolo, Oreste Organic Process Research and Development, 2002 , vol. 6, # 4 p. 379 - 383

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Citation Number: 52

Abstract

Tolterodine, an important urological drug, can be conveniently prepared starting from 1-[2- hydroxy-5-methyl) phenyl]-1-phenylethylene, accessible in high yield by alumina-promoted ortho alkenylation of p-cresol with phenylacetylene. The hydroformylation of this olefin, catalyzed by rhodium complexes both in homogeneous or in aqueous biphasic system, affords the desired linear aldehyde in about 80-90% yield. The reductive amination of this ...