2-(2-氨基噻唑-4-基)-2-三苯甲氧基亚氨基乙酸乙酯的全合成研究

Total synthesis of 2-(2-Aminothiazole-4-yl)-2-methoxyiminoacetic acetate

对2-(2-氨基噻唑-4-基)-2-三苯甲氧基亚氨基乙酸乙酯的合成工艺进行了研究。以乙酰乙酸乙酯为起始原料,合成去甲基氨噻肟酸乙酯。然后再与三苯基氯甲烷反应,得到2-(2-氨基噻唑-4-基)-2-三苯甲氧基亚氨基乙酸乙酯。并优化了反应条件,使总收率达到48.8%,高于现有文献值(35.3%)。2-(2-氨基噻唑-4-基)-2-三苯甲氧基亚氨基乙酸乙酯结构经核磁共振氢谱确证。改进后的合成路线操作简单,收率高,易于实现工业化。

The synthesis process of 2 - （2 - Aminothiazole - 4 - yl } - 2 - methoxyiminoacetic acetate was explored in this paper. Taking ethyl acetoacetate as source material, ethyl 2 - （ aminothiazol - 4 - yl） - 2 - hydroxyiminoacetate is synthesized , which reacts with tripheryl chloromethane to produce 2 - { 2 - aminothiazol - 4 - yl } - 2 - trityloxyiminoacetic acetate. The conditions of reaction are improved and the yield is 48.8 %, which is higher than any other current report （ 35.3 % ） can do. The structure of 2 - （ 2 - Aminothiazole - 4 - yl） - 2 - methoxyiminoacetic acetate was confirmed by H - NMR. A more reasonable operational path for the manufacturing process of 2 - （ 2 -Aminothiazole -4 -yl） -2 -methoxyiminoacetic acetate was provided by this experiment.