Direct Intermolecular N-H Aziridine Synthesis, an Emerging Methodology for Practical Synthesis

Abstract

An aziridine is a highly strained, triangular molecule that has been recognized as an invaluable synthetic intermediate as well as a structural motif of bioactive molecules. Numerous catalytic/stoichiometric, racemic/asymmetric methods for synthesis of N-protected aziridines have been demonstrated but a practical method for direct N-H aziridine synthesis has been missing for decades despite of its promising utility for drug design. The present review describes recent developments of intermolecular N-H aziridine synthesis as an emerging field of potential application to practical and stereoselective synthesis.