Efficient synthesis of functionalized 1,3-dihydroisobenzofurans from salicylaldehydes: Application to the synthesis of escitalopram

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.

Graphical abstractAn efficient synthesis of substituted 1,3-dihydroisobenzofurans is developed.Figure optionsDownload full-size imageDownload as PowerPoint slide