Nitrogen-atom insertion enables skeletal editing of pyrrolidines for tetrahydropyridazine synthesis

Abstract

In the July 17 issue of Science, Lu et al. disclose a strategy for converting abundant pyrrolidines into tetrahydropyridazines via a nitrogen-atom insertion process with O-diphenylphosphinyl hydroxylamine as the nitrogen source, providing a powerful platform for the rapid construction of a variety of nitrogen-containing diazacycles and the late-stage derivatization of drug-like molecules.