2-Picolylamine (I) is protected with Boc2O, and the resultant tert-butyl carbamate (II) is further alkylated with methyl 4-(bromomethyl)benzoate (III) to furnish (IV). Subsequent saponification of the methyl ester group of (IV) affords the carboxylic acid (V).

The protected arginine (VI) is coupled to (S)-1-naphthylethylamine (VII) in the presence of EDC/HOBt to give amide (VIII). Subsequent N-Fmoc group removal employing diethylamine in DMF leads to amine (IX), which is further condensed with carboxylic acid (V) yielding amide (X). Finally, trifluoroacetic acid-promoted cleavage of the N-Boc and N-Pbf protecting groups of (X) provides the title compound.