细胞凋亡激动剂β-拉帕醌的合成  

Synthesis of β-lapachone

作　　者：孙敏[1] 魏红涛[1] 蔡进[1] 吉民[1] 

机构地区：[1]东南大学化学化工学院制药工程系,南京210096

出　　处：《中国新药杂志》2008年第18期1598-1599,共2页Chinese Journal of New Drugs

摘　　要：目的:合成细胞凋亡激动剂β-拉帕醌。方法:以2-羟基-1,4-萘醌为起始原料,先制得中间体拉帕醇,再经浓硫酸环合得β-拉帕醌,结果:以总收率59.5%合成了细胞凋亡激动剂β-拉帕醌,结构经核磁氢谱(1HNMR)、质谱(MS)确证。结论:本合成路线反应条件温和,原料价廉易得,收率较文献有所提高。Objective ： To synthesize β-1apachone, an apoptotic agonist. Methods： Starting from 2-hydrox- y-1,4-napthoquinone, the lapachol was prepared, and then converted to β-lapacbone by treatment with concentrated sulfuric acid. Results： β-Lapachone was synthesized with the yield of 59.5%. The structure was verified by ^1HNMR and MS. Conclusion： A pragmatic synthesis procedure for β-lapachone is achieved with advantages of mild reactive condition and cheaper starting reagents. The yield of β-lapachone is much higher than ever reported.

关 键 词：β-拉帕醌 细胞凋亡激动剂 化学合成 

分 类 号：R979.1[医药卫生—药品]