A convenient and high yielding method for the preparation of (R)‐tolterodine, utilizing a catalytic asymmetric Me‐CBS reduction was developed. Highly enantioenriched (R)‐6‐methyl‐4‐phenyl‐3,4‐dihydrochromen‐2‐one (94% ee) was recrystallized to yield practically enantiopure material (ee >99%) and converted to (R)‐tolterodine in a four‐step procedure. The configuration of the crucial stereocenter was preserved during the synthesis and the obtained product was identified by chiral HPLC to be the (R)‐tolterodine enantiomer.
No takes yet. Share an insight, caveat, or question.
Hedberg et al. (2005) studied this question.
Synapse has enriched 5 closely related papers on similar clinical questions. Consider them for comparative context: