Efficient Ring-Closure Approach via Copper-Catalyzed Reactions of Sulfonyl Azide, Terminal Alkynes and Alcohols/Amines

We have developed a general and efficient method for synthesis of medium- and large-sized heterocycles via copper-catalyzed reactions of sulfonyl azide, terminal alkynes (or bisalkyne) and alcohols/amines (diamines) at room temperature, and the highly practical method provides an entry toward diverse medium- and large-sized heterocycles.