Abstract: As an excellent nucleophile, 1⁃hydroxytryptamine derivatives have been widely used in the synthesis in recent years. With the development of indole alkaloids, 1⁃hydroxytryptamine derivatives will play an important role in the future research. In this paper, 1⁃hydroxytryptamine derivatives were synthesized by tryptamine synthesis method with indole substituted by benzene ring as substrate, protection of nitrogen atom in side chain of tryptamine, reduction of indole ring and oxidation of nitrogen atom in indole ring. Finally, the synthesis of the 1⁃hydroxytryptamine derivative was completed in a medium or higher yield. By this method, we synthesized a series of 1⁃hydroxytryptamine derivatives, and confirmed the accuracy of the structure of the compounds by 1H⁃NMR and 13C⁃NMR.

Key words: 1?Hydroxytryptamine derivatives, Indole, Reduction, Oxidation

摘要： 1⁃羟基色胺衍生物作为一种良好的亲核试剂，在近些年的有机合成中被广泛应用。随着吲哚生物碱研究的兴起，1⁃羟基色胺衍生物会在今后的合成研究中起到重要的作用。以含有取代基的吲哚为底物，经过甲酰化反应、亨利反应、四氢铝锂还原反应、保护基取代反应、三乙基硅烷还原反应、过氧化氢（双氧水）氧化反应，最终以良好的收率完成了1⁃羟基色胺衍生物的合成。通过该方法，合成了一系列的1⁃羟基色胺衍生物，经1H⁃NMR及13C⁃NMR表征，确定了1⁃羟基色胺衍生物的结构。

关键词: 1?羟基色胺衍生物, 吲哚, 还原, 氧化