目的:采用酶拆分法合成L-2,6-二甲基苯丙氨酸和L-2,4,6-三甲基苯丙氨酸。方法:通过乙酰氨基丙二酸二乙酯氨基酸合成法合成外消旋N-乙酰-2,6-二甲基苯丙氨酸和N-乙酰-2,4,6-三甲基苯丙氨酸,再以L-氨基酰化酶拆分,制备L-2,6-二甲基苯丙氨酸和L-2,4,6-三甲基苯丙氨酸。结果:以乙酰氨基丙二酸二乙酯为起始原料,分别以87.9%和86.0%的收率合成了外消旋的2,6-二甲基苯丙氨酸和2,4,6-三甲基苯丙氨酸。氨基酰化酶能拆分DL-N-乙酰-2,6-二甲基苯丙氨酸得到L-2,6-二甲基苯丙氨酸,但对N-乙酰-2,4,6-三甲基苯丙氨酸没有水解活性。结论:L-氨基酰化酶能用于2,6-二甲基苯丙氨酸的拆分,不能用于2,4,6-三甲基苯丙氨酸的拆分。 OBJECTIVE: To synthesize L-2,6-dimethylphenylalanine and L-2,4,6-trimethylphenylalanine by enzymatic resolution. Methods: Racemic N-acetyl-2,6-dimethylphenylalanine and N-acetyl-2,4,6-trimethylphenylalanine were synthesized by the amino acid synthesis of diethyl acetamidomalonate Acid and resolving with L-aminoacylase to prepare L-2,6-dimethylphenylalanine and L-2,4,6-trimethylphenylalanine. Results: Racemic 2,6-dimethylphenylalanine and 2,4,6-dimethylphenylalanine were synthesized in yields of 87.9% and 86.0%, respectively, starting from diethyl acetamidomalonate. Trimethylphenylalanine. Aminoacylase cleaves DL-N-acetyl-2,6-dimethylphenylalanine to give L-2,6-dimethylphenylalanine, but N-acetyl-2,4,6 Trimethylphenylalanine has no hydrolytic activity. Conclusion: L-Aminoacylase can be used for the resolution of 2,6-dimethylphenylalanine and can not be used for the resolution of 2,4,6-trimethylphenylalanine.