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Synfacts 2009(11): 1181-1181  
DOI: 10.1055/s-0029-1218036
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart ˙ New York

Synthesis of (R)-Tolterodine

Contributor(s): Philip Kocienski
K. Yoo, H. Kim, J. Yun*
Sungkyunkwan University, Suwon, Korea
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Publication History

Publication Date:
22 October 2009 (online)

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Significance

(R)-Tolterodine is a muscarinic antagonist used for the treatment of urinary incontinence. Key steps in the short synthesis depicted are (1) a copper-catalyzed addition (hydroarylation) of phenylboronic acid to an alkynylnitrile (C → D) and (2) a CuH-catalyzed asymmetric conjugate reduction of an α,β-unsaturated nitrile (D → E).