Preparation | 1.5-aminopyrazine-2-methyl formate synthesis process, which is characterized in that it is prepared by the following synthesis steps: 5-halopyrazine-2-formate is used as raw material to react with substituted amininating reagents to generate 5-substituted aminopyrazine-2-formate, 5-substituted aminopyrazine-2-formate deamination protecting group and then hydrolysis of the ester to produce 5-aminopyrazine-2-formate; the specific steps are as follows:(1) 5-halogenated pyrazine-2-formate is used as raw material and substituted amination reagent in the presence of organic solvent and alkali Reacts at 60-70 ℃, after the reaction, the reaction liquid is poured into water, filter and dry to obtain methyl 5-aminopyrazine-2-formate, wherein X is any one of F,Cl,Br,l; wherein R is any one of methyl, ethyl, and isopropyl; R2 is any one of p-methoxybenzylamine or tert-butylamine; the molar ratio of the alkali to 5-halopyrazine-2-formate is 1.1:1; the molar ratio of the substituted aminidation reagent to 5-halopyrazine-2-formate is 1.5-2.0: 1;(2)5-substituted aminopyrazine-2-formate refluxing under the action of acid to generate an acid salt corresponding to methyl 5-aminopyrazine-2-formate, the acid is trifluoroacetic acid, hydrochloric acid, any one of hydrobromic acid; (3) 5-aminopyrazine-2-formic acid is used as an acid salt of 5-aminopyrazine-2-formate in the action of alkali to obtain 5-aminopyrazine-2-formic acid. The alkali is sodium hydroxide, and the molar ratio of sodium hydroxide to 5-aminopyrazine-2-formate is 2-3:1. |