A non-lithiation route towards facile synthesis of bioactive 4, 9-dimethoxynaphthalide

A simple, facile, and convenient route is adopted for the synthesis of 4,9-dimethoxynaphthalide (4,9-DMN); an analog of naturally occurring naphthalene lactone family. It is achieved without involving a tedious and hazardous lithiation step using 3-(bromomethyl)-1,4-dimethoxy-2-naphthaldehyde as key intermediate through base catalyzed oxidative cyclization resulting in a five-membered lactone ring. This compound exhibits significant anti-fungal activity againstCandida albicanswhile it is found to be less toxic towards MCF-7 cancer cell line with IC(50)value less than 250 mu M.