9. A Mannich-Cyclization Approach for the Asymmetric Synthesis of Saturated N-Heterocycles
A. Münch, B. Wendt, M. Christmann
A concise asymmetric synthesis of disubstituted N-heterocycles is reported. Our approach utilizes an optimized Mannich reaction of functionalized aldehydes, followed by a novel dehydrative cyclization mediated by the Staab reagent (1,1′-carbonyldiimidazole, CDI). The method was applied to the synthesis of azetidines, piperidines and pyrrolidines.