Direct Amidation of Carboxylic Acids with Nitroarenes.

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