Triazenyl Alkynes as Versatile Building Blocks in Multicomponent Reactions: Diastereoselective Synthesis of β‐Amino Amides

Multicomponent reactions (MCRs) are powerful tool for the construction of polyfunctional molecules in an operationally simple and atom‐economic manner, and the discovery of novel MCRs requests various building blocks. Herein, triazenyl alkynes were disclosed as versatile building blocks in a multicomponent reaction with carboxylic acids, aldehydes and anilines to furnish β‐amino amides with the achievement of high diastereoselectivity and structural diversity. In this process, triazenyl alkynes were bifunctional so that the alkyne moiety acts as C2 fragment and triazene serves as directing group to modulate the transition state thus achieving high diastereoselectivity, in consistence with DFT calculations. Furthermore, the triazenyl group also enables diverse late‐stage transformation. This protocol opens a new vision for the discovery of building block and rational design of MCRs. Triazenyl alkynes serve as versatile building blocks in multicomponent reactions for diastereoselective synthesis of β‐amino amides. The alkyne moiety acts as C2 fragment and the triazene group serves as directing group to modulate the transition state thus to achieve both chemical reactivity and diastereoselectivity. The triazene group also enables late‐stage transformation. Diverse β‐amino amides were rapidly assembled in an operationally simple and atom‐economic process.