Three L-tryptophan derivatives (S)-2-{4’’-[(1’’’,3’’’-dioxoisoindolin-2-yl)methyl]benzamido}-3-(1’ H-indol-3’-yl)propanoic acid (I), (S)-2-{4’’-[(1’’’,3’’’-dioxoisoindolin-2-yl)methyl]cyclohexanecarboxamido}-3-(1’ H-indol-3’-yl)propanoic acid (II) and (S)-2-[6’’-(1’’’,3’’’-dioxoisoindolin-2-yl)hexanamido]-3-(1’ H-indol-3’-yl)propanoic acid (III) were synthesized through amidation reaction with three hemostatic amine acids protected by phthalic anhydride, including, 4-(aminomethyl)benzoic acid, 4-(aminomethyl)cyclohexane-1-carboxylic acid and 6-aminohexanoic acid. The structures were confirmed by IR, MS and 1H NMR and 13C NMR. Two coagulating target proteins were reversely screened, and positively docked with L-tryptophan and three compounds through MOE, respectively. Blood concretion four items and plasma re-calcification time indicated that compounds I and III showed better coagulating activity with increasing concentration, while compound II showed dose-dependent activity.