In synthesizing novel derivatives of natural cyclic peptide ogipeptins, we established a simple and practical solid-phase peptide synthesis and macrocyclization method. By using this method, it became possible to obtain skeleton-modified ogipeptin derivatives with dehydroxylation of β-hydroxy-α,γ-diaminobutyric acid, replacement of Z-dehydrobutyrine residue, or replacement of arginine residue.