Luzopeptins are a series of cyclic depsipeptides which possesses potent antitumor and antiviral activities. There is no total synthesis of Luzopeptins has been achieved. In our own effort to synthesize the luzopeptins, we developed a concise and practical route to PCA, 86, and an efficient protocol to synthesize the mono-BOC, 181. A novel serinyl chloride was devised in conjunction with the formation of PCA-serine dipeptide derivatives, 164. All these methodologies were successfully applied to the synthesis of monomeric derivative of luzopeptin E\sb2, 288.* ftn*Please refer to the dissertation for diagram.