Solid-phase synthesis of aryl squaramides using Liebeskind–Srogl cross-coupling

Abstract

We present a method for the synthesis of aryl-substituted squaramides through the Liebeskind–Srogl cross-coupling reaction performed on solid support. This approach offers a unique application for the cross-coupling reaction, allowing for the rapid and efficient production of a diverse range of substituted analogs within a combinatorial framework. Through our technique, we successfully synthesized derivatives that were previously unattainable. Additionally, the optimized conditions have been effectively applied in a scale-up reaction. The derivatives show potential for the treatment of drug-resistant tuberculosis.