E0462

CRYSTAL STRUCTURE OF TOLTERODINE By B. Sellberg, Pharmacia & Upjohn , Uppsala, Sweden and I. Engstrm and L.-E. Tergenius. Institute of Chemistry, University of Uppsala, Uppsala, Sweden.

Tolterodine is a drug substance containing (+)-N,N-diisopropyl-3-(2-hydroxy-5-methylphenyl)-3-phenylprolylamine hydrogen L(+)-tartrate (C26H37NO7).The drug is used for the treatment of urinary frequency, urgency and/or urge incontinence. The synthesis of tolterodin L(+)-tartrate is a well established procedure.

The crystal structure of tolterodine L(+)-tartrate was determined from single crystal x-ray data at room temperature and 30 K. The structure is monoclinic with two formula units in the unit cell and all the atoms in the general position of the space-group P21. The unit cell dimensions at 30 K are a = 9.1759, b = 16.3965 ,c =12.9196Å , = 93.427o. In the final stage of the refinement the 3568 reflections recorded at 30 K were refined to an R-value of 4.0 %.