Rapid Synthesis of Functionalized Indenes, Triazoles, and Glucocorticoid Receptor Modulators by Sequential Multicatalysis Cascade Reactions

A general process for the synthesis of substituted indenes and 1,2,3-triazoles was achieved for the first time through a multicatalysis cascade reaction of 2-ethynylbenzaldehydes, CH acids, organic hydrides, and azides in the presence of a catalytic amount of L-proline/CuI/DIPEA. In this communication, we discovered the utilization of a single copper catalyst for two different reactions and shown synthetic application to the high-yielding synthesis of glucocorticoid receptor modulators.