In order to find better herbicidal activity and fungicidal activity of α-amino acid derivatives, we introduced furan rings and pyridyl groups to seven different α-amino acids to form a series of 14 novel α-amino acylamines derivatives via dicyclohexylcarbodiimide/4-dimethylaminopyridine(DCC/DMAP) coupling method. The structures of all the compounds prepared were confirmed by IR, LC/MS, 1H NMR, and elemental analysis. The herbicidal and fungicidal results show that some compounds containing glycine and valine substrate have good activities. In order to find better herbicidal activity and fungicidal activity of α-amino acid derivatives, we introduced furan rings and pyridyl groups to seven different α-amino acids to form a series of 14 novel α-amino acylamines derivatives via dicyclohexylcarbodiimide / 4-dimethylaminopyridine The structures of all the compounds for the preparation of confirmed precursors by IR, LC / MS, 1H NMR, and elemental analysis. The herbicidal and fungicidal results show that some compounds containing glycine and valine substrates have good activities.