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

利用Liebeskind-Srogl交叉偶联反应固相合成芳基方酰胺

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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.

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