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Enantioselective Synthesis of (R)-Tolterodine via CuH-Catalyzed Asymmetric Conjugate Reduction

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journal contribution
posted on 05.06.2009, 00:00 by Kihyun Yoo, Hyohyun Kim, Jaesook Yun
An efficient and highly enantioselective method for the preparation of (R)-tolterodine is described. The synthesis was performed by CuH-catalyzed asymmetric conjugate reduction of a β,β-diaryl-substituted unsaturated nitrile as a key step, which is prepared by a stereoselective hydroarylation of alkynenitrile with aryl boronic acid. The synthesis was accomplished without employing the protection−deprotection sequence.