Cross-dehydrogenative regioselective Csp³-Csp² coupling of enamino-ketones followed by rearrangement: an amazing formation route to acridine-1,8-dione derivatives

Org Biomol Chem. 2016 Mar 7;14(9):2706-15. doi: 10.1039/c5ob02655e.

Abstract

A new general method for the synthesis of acridine-1,8-diones through CDC coupling of enamino-ketones followed by rearrangement has been developed. This is a Cu(i) catalyzed procedure, based on the cross dehydrogenative coupling of the Csp(3)-H bond with the Csp(2)-H bond of enamino-ketones followed by rearrangement to acridine-1,8-diones in the presence of PTSA under an aerobic atmosphere. The synthetic route has been broadly applicable to a wide range of enamino-ketone derivatives derived from different benzyl amines as well as primary aliphatic amines having Cα(sp(3))-H bonds with various cyclic, acyclic 1,3-diketones and also using DEAD.

Publication types

  • Research Support, Non-U.S. Gov't