二甲氧基嘧啶胺合成工艺改进研究

Improved Synthesis of 2-Amino-4,6-Dimethoxy Pyrimidine

以硝酸胍和丙二酸二乙酯为原料,经过环合生成2-氨基-4,6-二羟基嘧啶,氯化生成2-氨基-4,6-二氯嘧啶,再经甲氧基化得最终产品2-氨基-4,6-二甲氧基嘧啶。得到了该3步合成过程的合适工艺条件,3步合成总的收率为81.3%,最终产品纯度为99.2%,熔点95℃。

Guanidine nitrate and diethyl malonate were used as main materials to prepare 2--amino--4, 6 --dicarboxyl pyrimidine by cyclization, followed by chloridization to prepare 2--amino--4, 6--dichloro- pyrimidine, and then by methoxidization to prepare 2--amino--4, 6--dimethoxy pyrimidine. The suitable reaction conditions of these processes have been obtained. The overall yield of the end product was 81.3%. The purity of the end product was 99.2%, and m. p. was 95℃.