Recent Advances in the Synthesis of Nitrogen Heterocycles Using β-Nitrostyrenes as Substrates

Abstract:: The exploration of synthetic methodologies that allow rapid access to a wide variety of N-heterocycles is of critical importance to the medicinal chemist as it provides the ability to expand the available drug-like chemical space and drives more efficient drug discovery programs. β-Nitrostyrenes, as unique active intermediates, have been widely applied in synthetic organic chemistry because of their versatile utility as pharmaceutical agents and agrochemicals. In this review, we summarize the recent development and application of the elegant and efficient methods that enable the concise synthesis of N-heterocycles from β-nitrostyrenes and various partners in a step- and atom-economic manner, including cascade reactions, C-H activation, regio- and stereoselective syntheses, as well as other novel syntheses, which will potentially provide useful insights for further exploring and designing novel reactions.