2,5-二甲氧基苯乙胺的合成

Synthesis of 2,5-Dimethoxy Phenethylamine

选取了一条合理、成本相对低廉的合成2,5-二甲氧基苯乙胺新方法。在碱性条件下,对苯二酚经醚化得到1,4-二甲氧基苯,收率95.0%,再选用高选择性的溴化剂溴化后,收率90.0%,经格氏反应和羟乙基化反应制备2,5-二甲氧基苯乙醇,收率75.0%,醇与对甲苯磺酰氯反应得到酯,收率97.0%,最后经Gabriel反应可以制备相应的芳香乙胺化合物,收率70.0%。该路线反应较易,条件温和,对设备要求较低,原料价廉易得,适合工业生产。

A new route to produce 2,5-dimethoxy phenethylamine was introduced in the paper. Under the basic condition, 1,4-dihydroxy benzene was reacted with dimethyl sulfate to get 1,4-dimethoxy benzene with 95.0% of the yield. 1,4-dimethoxy benzene was brominated with high-selective bromating agent to produce 1,4-dimethoxy benzene bromide with 90% of yield. 2,5-dimethoxy phenethanol was synthesized from 1,4-dimethoxy benzene bromide through Grignard reaction and hydroxyethylation （the yield 75.0%）, and esterification （the yield 97.0%） and Gabriel reaction （the yield 70.0%） . Though there are five steps in this route, but the conditions are mild and easy to carry out, so it is of extensive industrial perspective.