Copper(I)‐Catalyzed Four‐Component Interrupted Click/Amination: Efficient Synthesis of Fully Substituted 5‐Amino‐1,2,3‐Triazoles

ABSTRACT A copper(I)‐catalyzed four‐component interrupted click/amination cascade reaction for the efficient synthesis of various 5‐amino‐1,2,3‐triazoles has been developed. The key step in this reaction is the interception of the in situ‐formed cuprate‐triazole intermediate with O ‐benzoylhydroxylamine. This four‐component reaction proceeds under mild conditions with complete regioselectivity. It's also characterized by a broad substrate scope and good functional group tolerance.