The synthesis of a cyclic fragment of homophymine B is described. Fmoc-derivatives of βMOT and AHDH, which were necessary unusual amino acids for a designed cyclic depsipeptide, were prepared. The linear peptides were synthesized using Fmoc-based solid phase peptide synthesis. The designed cyclic depsipeptide was constructed via the macrolactamization between the Pip and d-Asp residues of the corresponding linear peptide with PyBOP/HOAt/DIPEA in DMF followed by global deprotection to give the cyclic fragment of homophymine B.