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A facile one-pot synthesis of 2-styrylindoles, through Suzuki arylation of ortho-substituted chloroenynes followed by N-cyclization and N-demethylation, has been developed. A variety of 2-styrylindoles were obtained in good to excellent yields and were evaluated for their anticancer properties.

One-Pot Synthesis of 2-Styrylindoles from Ortho-Substituted Chloroenynes