2-氨基-4,6-二氯-5-甲酰胺基嘧啶的合成工艺研究

Synthesis of N-(2-amino-4,6-dichloro-5-pyrimidinyl) formamide

目的优化硫酸阿巴卡韦中间体2-氨基-4,6-二氯-5-甲酰胺基嘧啶。方法以氨基丙二酸二乙酯盐酸盐和碳酸胍为原料,经过环合、Vilsmeier两步反应,制备2-氨基-4,6-二氯-5-甲酰胺基嘧啶。结果合成了2-氨基-4,6-二氯-5-甲酰胺基嘧啶,收率82.62%,纯度99.62%。结论通过该研究,获得了一条高效、简洁的2-氨基-4,6-二氯-5-甲酰胺基嘧啶制备路线,有工业化应用前景。

Objective To optimize the synthetic procedure of N-（2-amino-4,6-dichloro-5-pyrimidiyl）formamide as the intermediate of Abacavir Sulfate.Methods N-（2-amino-4,6-dichloro-5-pyrimidiyl）formamide was prepared by cyclization and Vilsmeier reactions of dietylaminomalonate hydrochloride and guanidine carbonate.Results N-（2-amino-4,6-dichloro-5-pyrimidinyl）formamide was synthesized with yield（82.62%）and purity（99.62%）.Conclusions An efficient,concise synthesis route with the industrial perspective of N-（2-amino-4,6-dichloro-5-pyrimidinyl）formamide is available.