Copper(i)-catalysed intramolecular hydroarylation-redox cross-dehydrogenative coupling of N-propargylanilines with phosphites

Abstract

Intramolecular hydroarylation-redox cross-dehydrogenative coupling of N-propargylanilines with phosphite diesters proceeded in the presence of Cu(I)-catalysts (20 mol%) to selectively give 2-phosphono-1,2,3,4-tetrahydroquinolines in good yields with 100% atomic utilization. P–H and two C–H bonds are activated at once and these hydrogen atoms are trapped by a propargylic triple bond in the molecule.