The invention discloses L-leucine derivatives blocking the entrance of H5N1 avian influenza virus, which are 3,4-dyhydroxyl benzoyl leucine methyl ester and 3,4-dyhydroxyl phenylacetyl leucine methyl ester. The 3,4-dyhydroxyl benzoyl leucine methyl ester is prepared by condensing 3,4-dyhydroxyl benzoic acid with L-leucine methyl ester; the 3,4-dyhydroxyl phenylacetyl leucine methyl ester is prepared by taking 3,4-dyhydroxyl phenylacetic acid as a starting material, treating the 3,4-dyhydroxyl phenylacetic acid by virtue of dimethyl sulphate and thionyl chloride sequentially, then condensing the 3,4-dyhydroxyl phenylacetic acid with L-leucine methyl ester, and then performing demethylation reaction. The compounds, namely, the 3,4-dyhydroxyl benzoyl leucine methyl ester and the 3,4-dyhydroxyl phenylacetyl leucine methyl ester, disclosed by the invention, have a strong inhibitory activity on Influenza strain A/Vietnam/1194/2004 avian influenza virus, and have a mechanism of acting on the entrance phase of H5N1 virus infected cells; and the compounds are a new inhibitor resisting the entrance of avian influenza virus, and can be used as a medicine for preventing or treating H5N1 avian influenza.