Described herein is a convergent asymmetric synthesis of growth hormone secretagogue (GHS) suitable for large-scale preparations. Key features include:(1) an improved method for α-iodination of a lactam;(2) a novel synthesis of a disubstituted urea using Ti (Oi-Pr) 4 and NaBH4;(3) construction of biphenyl ureas via an unprecedented Suzuki coupling;(4) an in situ mesylation/N-alkylation of a benzolactam.