Aryne Reaction and Cross-coupling Approach for the Synthesis of Diverse N-Arylphenylalanine Derivatives

A facile synthesis of diverse N-arylphenylalanine derivatives is described. We have developed an efficient method for preparing diverse N-arylphenylalanine ester-type platforms containing an aryne generating moiety and a halogen via oxidative cross-coupling. A wide variety of N-arylphenylalanine esters were convergently synthesized using the platforms by a range of aryne reactions and following cross-coupling reactions.