Enantioselective intramolecular propargylic amination using chiral copper-pybox complexes as catalysts

Intramolecular propargylic amination of propargylic acetates bearing an amino group at the suitable position in the presence of chiral copper-pybox complexes proceeds enantioselectively to give optically active 1-ethynyl-isoindolines (up to 98% ee). The method described in this communication provides a useful synthetic approach to the enantio-selective preparation of nitrogen containing heterocyclic compounds with an ethynyl group at the alpha-position.