论文部分内容阅读
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:Synthesis of L-2,6-dimethylphenylalanine and L-2,4,6-trimethylphenylalanine through enzymatic resolution.Methods:Racemic 2,6-dimethylphenylalanine and 2,4,6-trimethylphenylalanine were synthesized through reaction of diethyl acetamidomalonate with 2,6-dimethylbenzyl bromide or 2,4,6-trimethylbenzyl bromide,respectively.The DL-amino acids were then enzymatically resoluted by L-amino acylase.Results:Racemic 2,6-dimethylphenylalanine and 2,4,6-trimethylphenylalanine were synthesized through reaction of diethyl acetamidomalonate with 2,6-dimethylbenzyl bromide and 2,4,6-trimethylbenzyl bromide in yield of 87.9% and 86.0% respectively;DL-2,6-dimethylphenylalanine was successfully resoluted by L-amino acylase,but it was failed in the resolution of 2,4,6-trimethylphenylalanine.Conclusion:L-amino acylase can be used in the resolution of DL-2,6dimethylphenylalanine,but it is ineffective in the resolution of 2,4,6-trimethylphenylalanine.