Alkylation of 2-(Boc-amino)caprolactam (I) with 4-(bromomethyl)biphenyl (II) in the presence of KOH and tetrabutylammonium iodide produced the N-(biphenylylmethyl) lactam (III). After Boc group cleavage with trifluoroacetic acid, the resulting amino lactam (IV) was coupled with the tyrosine derivative (V) using BOP to furnish the corresponding amide.