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Synfacts 2011(7): 0696-0696  
DOI: 10.1055/s-0030-1260481
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart ˙ New York

Asymmetric Synthesis of (R)-Tolterodine

Contributor(s): Philip Kocienski
X. Wang*, A. Guram, S. Caille, J. Hu, J. P. Preston, M. Ronk, S. Walker
Amgen Inc., Thousand Oaks, USA
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Publication History

Publication Date:
17 June 2011 (online)

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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.