The synthesis of DL-Tfm was performed in six steps, starting with commercially available Lhomocystine. The general strategy was to protect the amine and carboxylate with Boc group and benzyl group respectively, then reduce the disulfide with phosphine reagent, trifluoromethylation of the exposed free thiolate with Umemoto's reagent in the presence of base afforded the protected DL-Tfm. Final deprotection and subsequent ion exchange chromatographic purification gave DL-Tfm.