Abstract

AbstractPiperidine derivatives are highly abundant in natural products and pharmaceutically relevant compounds. Aza‐Prins cyclization has emerged as a step‐ atom‐economical and stereoselective method for the preparation of such azacycles. The possibility of coupling aza‐Prins process with the formation of a second cycle in a one‐pot manner is even more powerful and makes the object of this review. Cascade/domino/tandem bis‐cyclizations involving an aza‐Prins process, for the rapid construction of complex small molecules, are discussed in detail.

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