Abstract

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(O i-Pr) 4 and NaBH 4; (3) construction of biphenyl ureas via an unprecedented Suzuki coupling; (4) an in situ mesylation/ N-alkylation of a benzolactam.

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