Enantioselective synthesis of (s)- and (R)-tolterodine by asymmetric hydrogenation of a coumarin derivative obtained by a Heck reaction.

An efficient and short enantioselective synthesis of (S)- and (R)-tolterodine was performed by asymmetric hydrogenation of a coumarin intermediate, easily obtained by a Heck reaction from inexpensive and commercially available starting materials.