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Concise Formation of 4-Benzyl Piperidines and Related Derivatives Using a Suzuki Protocol

Susan Vice*, Tom Bara, Annette Bauer, C. Anderson Evans, Jennifer Fort, Hubert Josien, Stuart McCombie, Michael Miller, Dennis Nazareno, Anandan Palani and Jay Tagat

*Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, New Jersey, 07033-0593, Email:

S. Vice, T. Bara, A. Bauer, C. A. Evans, J. Fort, H. Josien, S. McCombie, M. Miller, D. Nazzareno, A. Palani, J. Tagat, J. Org. Chem, 2001, 66, 2487-2492.

DOI: 10.1021/jo0007682 (free Supporting Information)

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An efficient method of constructing 4-benzyl piperidines and related substances is described. This protocol tolerates a wide variation in both reaction partners and allows the concise formation of a variety of building blocks.

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Key Words

Hydroboration, Suzuki Coupling, Arenes

ID: J42-Y2001-540