药物化学

Nitroarenes are Synthesised by Oxidising Arylamines

Abstract

Antonella Tanini*

Nitro compounds are a type of organic molecule that has a wide range of applications in organic synthesis, medicinal chemistry, and materials science. The direct oxidation of primary amines is an appealing alternative route among the various methodologies available for their synthesis. Efforts to develop oxidative procedures for the synthesis of nitro derivatives have spanned decades, yielding a wide range of protocols for the selective oxidative conversion of amines to nitro derivatives. This review summarises methods for the synthesis of nitroarenes via aryl amine oxidation, with a focus on recent advances in the field. The harsh reaction conditions, as well as the poor functional group tolerance and regioselectivity, are the main drawbacks of this route. Many aromatic nitro derivatives are still difficult to synthesise via this method. Alternative nitration reagents and methodologies, including transition-metal-catalyzed ipso-nitration methodologies, have emerged as powerful tools for nitroarenes synthesis.