2-氨基-N-(2,2,2-三氟乙基)乙酰胺的合成

The synthesis of 2-amino-N-(2,2,2-trifluoroethyl)acetamide

在低温和碱性条件下,将甘氨酸与碳酸二叔丁酯反应制得N-(叔丁氧羰基)甘氨酸化合物(1).再将化合物1在N,N’-二环己基碳化二亚胺和4-二甲氨基吡啶的作用下与三氟乙胺盐酸盐进行酰胺化制得N-[2-氧代-2-[(2,2,2-三氟乙基)氨基]乙基]氨基甲酸-1,1-二甲基乙酯(2).然后将化合物2在盐酸作用下脱除保护基Boc,得到2-氨基-N-(2,2,2-三氟乙基)乙酰胺.最后通入氯化氢气体制成2-氨基-N-(2,2,2-三氟乙基)乙酰胺盐酸盐(3).化合物1~3经MS、IR、1 H NMR和13 C NMR等确证结构.文中所采用的方法具有原料易得、操作简便、安全性高等优点.

Compound 1 was synthesized by the reaction of glycine with （Boc）2O under low temperature and alkaline conditions. Compound 2 was obtained by acylation of compound 1 with 2,2,2-trifluoroethylamine hydrochloride in dichloromethane, using DCC as coupling agent and DMAP as catalyst. Reaction of compound 2 with hydrochloric acid to remove the protecting group Boc to give 2-amino-N （2,2, 2-trifluoroethyl） acetamide, and then was treated with hydrogen chloride gas to produce the hydrochloride salt 3. All compounds 1-3 were fully characterized by MS, IR, 1H NMR and 13C NMR. The method is easy to operate, has high safety and the raw materials are easily obtained.