Abstract An efficient synthesis of substituted 1, 3-dihydroisobenzofurans is developed. In this novel route, o-aroylbenzaldehydes, as key intermediates, can be obtained by lead tetraacetate oxidation of N-aroylhydrazones of salicylaldehydes. The mild and general strategy enables the synthesis of various substituted 1, 3-dihydroisobenzofurans in high yields. Moreover, this method can be applied to efficiently synthesize escitalopram.