以碳酸钠为缚酸剂,摩尔比为1:1的2,6-二甲基苯胺与氯乙酰氯反应合成了中间体2-氯-N-(2,6-二甲基苯基)乙酰胺;在强碱乙醇钠作用下,2.吡咯烷酮再与2-氯.N-(2,6-二甲基苯基)乙酰胺经亲核取代合成了目标化合物奈非西坦。探讨了影响中间体和奈非西坦产率的因素,在乙醇钠、2.氯-N-(2,6-二甲基苯基)乙酰胺和2-吡咯烷酮的摩尔比为2:1:2、反应时间为2h的较佳工艺条件下,产品总收率达81%。
The 2-chloro-N-(2,6-dimethyl) phenyl acetamide was obtained from 2,6-dimethylaniline and chloroacetyl (molar ratio of 1 1) using sodium carbonate as antacid agent. Then sodium ethoxide was used as base, the nucleophilic substitution of 2-pyrrolidone with the intermediate provided nefiracetam. The influencing factors of the reaction yield were studied. The optimum reaction conditions were as follows: n(ethanol sodium) : n(2-chloro-N-(2,6-dimcthyl)phenyl acetamide) : n(2-pyrrolidonc) was 2 : 1 : 2 and reaction time was 2 h. The total yield of the product was 81%.