Abstract

Using continuous-flow techniques, a small collection of 2<i>H</i>-azirines was prepared from oxime precursors via mesylation and base-promoted cyclisation. The 2<i>H</i>-azirines were either isolated after in-line purification or derivatised into a selection of 2-substituted aziridines through a telescoped reaction sequence involving nitrile, trifluoromethyl, or hydride nucleophilic addition. Importantly, these 2-substituted aziridines were produced with high <i>cis</i> diastereoselectivity providing access to small chiral heterocyclic entities that hold promise for medicinal chemistry programs because of their druglike features.

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