A convenient synthesis of activated enantiomerically pure 2- ethynylaziridines

Article abstract of DOI:10.1016/S0957-4166(98)00406-6

2,3-cis- and 2,3-trans-N-Arylsulfonyl-2-ethynylaziridines with high enantiomeric purity have been synthesized. N-Protected amino aldehydes synthesized from natural α-amino acids were successively treated with Ph₃P=C(Br)CO₂Me, DIBAL, MsCl-Et₃N, NaH in DMSO, and tert-BuOK in THF to yield 2-ethynylaziridines in good to high yields.