Abstract
An efficient stereoselective synthesis of trans-1-aryl-2-aminotetralins has been achieved via Cu(OTf) 2 catalyzed one-pot aziridination and regioselective intramolecular arylation of in situ generated aziridines from 2-arylethyl styrenes and PhINSO 2(4-NO 2C 6H 4) [PhINNs]. Reaction of a mixture of E/ Z-styrenes (⩽85:15) provided trans-N-protected-1-aryl-2-aminotetralins with high diastereoselectivity (dr > 95:5), which are important synthons for many artificial pharmaceuticals.
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