以2-氨基吡嗪(Ⅰ)为原料,经溴代、吗啉取代,合成得到目标化合物2-氨基-5-溴-3-吗啉-4-基吡嗪(Ⅲ),合成路线总收率为45.9%(以2-氨基吡嗪计),目标化合物结构经1HNMR确证。该文对反应投料比、温度、反应时间等因素进行了考察并优化,最优反应条件为:n(2-氨基吡嗪)∶n(溴素)∶n(吡啶)=1∶2.1∶2.1,避光,40℃下反应30 min;每克3,5-二溴-2-氨基吡嗪加入4 mL吗啉,80℃下反应1 h。优化后的合成路线反应条件温和、操作简单、成本低廉,适合较大规模制备。 The target compound 2-amino-5-bromo-3-morpholin-4-ylpyrazine (Ⅲ) was synthesized by substituting 2-aminopyrazine (Ⅰ) The rate of 45.9% (2-aminopyrazine), the target compound structure confirmed by 1HNMR. The reaction conditions such as feed ratio, temperature, reaction time and other factors were investigated and optimized. The optimal reaction conditions were as follows: n (2-aminopyrazine): n , Protected from light and reacted at 40 ° C for 30 min; 4 mL of morpholine was added per gram of 3,5-dibromo-2-aminopyrazine and reacted at 80 ° C for 1 h. Optimized synthesis route mild reaction conditions, simple operation, low cost, suitable for large-scale preparation.