Direct Amidation of Carboxylic Acids with Nitroarenes

• DOI: 10.1021/acs.joc.9b02068
• Publication Date: 2019-10-08T10:26:32Z
• Authors: Shao-Peng Wang; Chi Wai Cheung; Jun-An Ma
• Keywords: Amide; Agrochemical

N-Aryl amides are an important class of compounds in pharmaceutical and agrochemical chemistry. Rapid low-cost synthesis N-aryl remains high demand. Herein, we disclose operationally simple process to access directly from readily available nitroarenes carboxylic acids as coupling substrates. This method involves the situ activation acyloxyphosphonium salt for one-pot amidation, without need isolation corresponding synthetic intermediates. Furthermore, ease preparation workup allow quick efficient a wide range amides, including several amide-based druglike molecules.