The antiviral drug, lopinavir, was prepared Lopinavir was synthesized from (2S, 3S, 5S)-5-tert-Butyloxycarbonylamino-2-amino-3-hydroxy-1, 6-diphenylhexane reaction with 2, 6-Dimethylphenoxyacetic acid by condensation deprotection, which was subjected to condensation with (2S)-(1-Tetrahydropyramid-2-one)-3-methylbutanoic acid. The target product was synthesized via three-step procedure starting from BDC in a total yield of 50.7% and its structure was confirmed by 1H-NMR, ESI-MS. The method of preparation was much easier to perform, with simple work-up and fewer byproducts. It is suitable for industrial production