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A modified and improved procedure has been developed for the preparation of chiral nonracemic N-tosyl-2-alkyl aziridines in a single step starting from readily available β-amino alcohols. The procedure relies on a one pot N-tosylation/O-tosylation/intramolecular SN displacement, which furnishes the target heterocycles in excellent yields. The application of this protocol on a multigram scale has also been explored with excellent results. In addition, the application of a similar methodology has also allowed the preparation of N-benzyl-2-alkyl aziridines.

An improved procedure for the preparation of chiral nonracemic N-tosyl-2-alkylaziridines and N,2-dialkylaziridines on multigram-scale