SnAP Reagents for the Synthesis of Piperazines and Morpholines

Substituted piperazines
and morpholines are valuable structural
motifs in biologically active compounds, but are not easily prepared
by contemporary cross-coupling approaches. In this report, we introduce
SnAP reagents for the transformation of aldehydes into N-unprotected piperazines and morpholines. This approach offers simple,
mild conditions compatible with aromatic, heteroaromatic, aliphatic,
and glyoxylic aldehydes and provides mono- and disubstituted N-heterocycles
in a single step.