Asymmetric Synthesis of (R)-Tolterodine

Significance

A new asymmetric hydrogenation of 1,1-diarylethenes has been applied to the synthesis of (R)-tolterodine (Detrol^♦), an antimusca­rinic drug widely prescribed for the treatment of urinary incontinence. The key reaction employs a cationic rhodium catalyst and a range of different diphosphine ligands to deliver 1,1-diarylalkane derivatives in high yields and enantioselectivities.