N -Arylation of Amino Acid Esters via an I 2 -Mediated Metal-Free Multicomponent Benzannulation Strategy.

Herein, we present a novel method for the N -arylation of amino acid esters using α-bromoacetaldehyde acetal and acetoacetate via an I 2 -mediated metal-free benzannulation strategy, which disclosed the first synthetic application of N -arylation of amino acids using nonaromatic building blocks. The synthesized N -arylated amino acid derivatives were found to possess promising selective inhibition against human hepatocellular liver carcinoma cells, human melanoma cells, and human normal liver cells, with an IC 50 value as low as 16.79 μg·mL -1 .