2-氨基-4,6-二甲氧基嘧啶的合成工艺改进
Improved Synthesis of 2-Amino-4,6-Dimethoxypyrimidine

本文以硝酸胍和丙二酸二乙酯为起始原料，在醇钠的碱性条件下发生环化反应生成2-氨基-4,6-二羟基嘧啶，再通过在N,N-二甲基苯胺催化条件下，与三氯氧磷发生反应，氯化得到2-氨基-4,6-二氯嘧啶，最后再与甲醇钠发生甲氧基化反应得到目标化合物2-氨基-4,6-二甲氧基嘧啶，收率84.97%。目标化合物HPLC纯度为99.8%。试验通过探讨反应条件对目标化合物的产率和纯度的影响，优选出最佳的反应条件，获得了一个环保，成本低廉，操作简单，反应条件温和，适合于工业化的生产工艺。
By using Guanidine nitrate and Diethyl malonates starting material, and 2-amino-4,6-dihydroxypyrimidine was obtained by cyclization reaction under the basic condition of sodium alcohol. Then 2-amino-4,6-dichloropyrimidine was obtained by 2-amino-4,6-dihydroxypyrimidine chlorination reaction with phosphorus oxychloride under the catalysis of N,N-dimethylaniline. Finally, 2-amino-4,6-dichloropyrimidine was obtained by methoxylation with sodium methoxide. The total yield was 84.97%. The purity of the target compound was 99.8%. By discussing the effect of reaction conditions on the yield and purity of target compounds, the best reaction conditions were selected to save energy, reduce costs, mild reaction conditions, simple operation, suitable for industrial production.