Diastereoselective synthesis of 4-hydroxytetralones via a cascade Stetter-aldol reaction catalyzed by N-heterocyclic carbenes

J Org Chem. 2010 Jan 1;75(1):273-6. doi: 10.1021/jo902376t.

Abstract

A cascade Stetter-aldol reaction of phthalaldehyde and Michael acceptors catalyzed by N-heterocyclic carbenes was developed. The corresponding 3-substituted-4-hydroxytetralones were obtained in moderate to good yields with good trans-selectivities. On the contrary, the separated Stetter reaction followed by aldol reaction gave 3-substituted-4-hydroxytetralones with good cis-selectivity. Oxidation or dehydration of the resulted 4-hydroxytetralone gave the corresponding naphthalenediol or naphthol derivative, respectively, in good yield.