Copper-Catalyzed N1 Coupling of 3-Aminoindazoles and Related Aminoazoles with Aryl Bromides

The N-1-selective arylation of 3-aminoindazoles using copper catalysis is herein reported. The reaction uses readily accessible aryl bromides as coupling partners, including those from heterocycles, and allows easy access to a broad variety of substituted 3-aminoindazoles. The methodology was also examined on other aminoazoles of interest for the pharmaceutical industry.

Automated summary

This study presents a copper-catalyzed method for the N-1-selective arylation of 3-aminoindazoles using readily accessible aryl bromides as coupling partners, facilitating the synthesis of a variety of substituted 3-aminoindazoles. The methodology was also applied to other aminoazoles of interest to the pharmaceutical industry.