CuI Catalyzed Synthesis of Sulfonated Propargylamines

ABSTRACT We report herein the synthesis of highly functionalized sulfonated propargylamines via a three‐component coupling reaction involving aldehyde, amine and sulfonated terminal alkynes in presence of a copper (I) catalyst. This reaction is effectively applicable to a variety of benzaldehydes as well as cyclic, acyclic, and benzylic amines. Due to their high degree of functionalization, the resulting sulfonated propargylamines serve as valuable building blocks for the direct synthesis of nitrogen containing natural products and complex amine derivatives.