褪黑激素的合成与表征

Synthesis and Characterization of Melatonin

以吲哚为起始原料,经4步反应合成了褪黑激素(MLT) 吲哚(1)在甲醇中羟基化得到5-羟基吲哚(2),(2)同2-氯乙胺在乙酸乙酯中进行胺乙基化反应得到5-羟基色胺(3),(3)与硫酸二甲酯在甲苯中对羟基进行醚化,得到5-甲氧基色胺(4),(4)经乙酰化得到产物MLT,收率80%

The title compound was prepared by a four-step reaction route with indole as a main starting material. Indole (1) was hydroxylated in methanol to give 5-hydroxyindole (2) in 71 % yield. Compound (2) reacted with 2-chloride ethylamine in ethyl acetate to give serotonin (3) in 73 % yield, and compound (3) reacted with dimethyl sulfate in toluene to give 5-methyoxytryptamine (4) in (78 %) yield, and compound (4) was acetylated to give the title compound MLT in 80 % yield.