Capsules for Automated Azide–Alkyne Click Reactions

The development of an automated and reproducible process for copper-mediated click reactions of alkynes and azides into 1,4-disubstituted 1,2,3-triazole products is described. This method utilizes prepacked capsules that contain all necessary reagents and materials for the reaction and purification processes. The reaction and product isolation steps are fully automated with no further user involvement, resulting in the triazole products in high purity. The effectiveness of capsule-based automated organic synthesis was further demonstrated by sequencing the automated synthesis of organic azides, followed by a second capsule for CuAAC with no intermediate purification.