Biaryl Peptides from 4-Iodophenylalanine by Solid-Phase Borylation and Suzuki-Miyaura Cross-Coupling

Resin-bound phenylalanine boronates were prepared by solid-phase Miyaura borylation of 4-iodophenylalanine peptides. Subsequent arylation through a Suzuki-Miyaura cross-coupling was carried out using a variety of aryl halides under conventional heating and under microwave irradiation. Microwaves greatly enhanced the arylation, shortening the reaction time and providing the biaryl peptides in higher purities.