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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.

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