新型催眠药褪黑激素的合成  

Synthesis of melatonin-a new sleeping drug

作　　者：何炜[1] 李晓晔[1] 张邦乐[1] 李仲杰[2] 

机构地区：[1]第四军医大学基础部化学教研室,陕西西安710033 [2]西北大学化学系

出　　处：《第四军医大学学报》2000年第8期949-951,共3页Journal of the Fourth Military Medical University

摘　　要：目的　研究适合工业化生产褪黑激素的合成工艺 .方法　由邻苯二甲酰亚胺成盐 ,氮烷基化 ,碳烷基化后经由Japp- Klingem an反应和 Fischer吲哚合成法关环 ,脱羧脱保护后得 5 -甲氧基色胺 ,乙酰化后得褪黑激素 .结果　以比文献高出 2 0 %的收率合成目标物 ,产品经质量鉴定 ,达到药用标准 .结论　该法操作简便 ,生产设备投资低 ,成本小 。AIM To study and look for a practical synthetic technique for industrial production of melatonin. METHODS K phthalimide (I) was prepared by phtalimide to generate N (3 brompropyl) phtalimide(II) and ethyl 2 acelyl 5 phthalimido pentanotate(III). Via 'Japp Kligeman' reaction and 'Fisher reaction', 2 ethoxycarboxyl 3 (2 phthalimido ethyl) 5 methoxy indole (V) was prepared. After saponification, hydrolysis, decarboxylation of V, 5 methoxy trypytamin (IV) was obtained. IV was acetelized to give melatoin (VII). RESULTS The total yield was 20% higher than the reported yield and the quality of product was up to the pharmacy standard. CONCLUSION The results of the present study indicate that the method is practical and cost efficient.

关 键 词：褪黑激素 合成 新型催眠药 

分 类 号：TQ467[化学工程—制药化工]