A one-pot direct transformation to remotely CÀH alkene functionalized 2-aryl benzoxazoles from the reaction of amidophenol and electronically deficient olefin was reported. Control experiments confirm that the Pd-catalyzed regioselective CÀH activation/alkenylation occurs at the first step by leading to ortho-alkenylated amidophenol; which subsequently underwent tandem intramolecular annulation to afford C4-alkenylated 2arylbenzoxazole derivatives.

A Pd-catalyzed aerobic approach to access C4-aryl benzoxazoles by tandem C–H ortho-arylation and acid-mediated annulation of 2-amidophenol has been presented.

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Iron(III) chloride mediated para-selective CÀ H chlorination and subsequent annulation of 2amidophenol to synthesize C5-and C5, C7-chlorinated benzoxazoles was developed. Further, the oxidative cross-dehydrogenative coupling of amidophenol with anisole by ferric chloride was explored to achieve the remotely anisylated benzoxazoles.

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