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Synfacts 2011(3): 0285-0285  
DOI: 10.1055/s-0030-1259472
Metal-Catalyzed Asymmetric Synthesis and Stereoselective Reactions
© Georg Thieme Verlag Stuttgart ˙ New York

Stereoselective Synthesis of Substituted Piperidin-4-ols

Contributor(s): Mark Lautens, Norman Nicolaus
L. Cui, C. Li, L. Zhang*
University of California, Santa Barbara, USA
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Publication History

Publication Date:
16 February 2011 (online)

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Significance

The piperidine core is an important substructure, which can be found in various natural products and medicinally relevant molecules. Due to this fact the development of selective and modular synthetic methods towards the piperidine scaffold is a desirable task. This paper presents a one-pot synthesis of piperidin-4-ols 2 starting from readily available N-homopropargyl amides of type 1 in high yields and good to excellent diastereoselectivities.