AlCl3•6H2O-Catalyzed Friedel-Crafts Alkylation of Indoles by the para-Quinone Methide Moiety of Celastrol

被引：7

作者：

Zhu, Yi ^{[1
]}

Chen, Ziwen ^{[1
]}

Huang, Zhenfei ^{[1
]}

Yan, Siwei ^{[1
]}

Li, Zhuoer ^{[1
]}

Zhou, Hu ^{[1
]}

Zhang, Xiaokun ^{[1
,2
]}

Su, Ying ^{[1
,2
]}

Zeng, Zhiping ^{[1
]}

机构：

[1] Xiamen Univ, Sch Pharmaceut Sci, Fujian Prov Key Lab Innovat Drug Target Res, Xiamen 361102, Peoples R China

[2] Sanford Burnham Prebys Med Discovery Inst, 10901 N Torrey Pines Rd, La Jolla, CA 92037 USA

来源：

MOLECULES | 2017年 / 22卷 / 05期

关键词：

celastrol; indole; Friedel-Crafts alkylation; AlCl3 center dot 6H(2)O; BIOLOGICAL EVALUATION; DERIVATIVES; DESIGN; ACID; ACTIVATION; FORMULATION; KINASE;

D O I：

10.3390/molecules22050742

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A classical Friedel-Crafts alkylation of different indoles catalyzed by AlCl3 center dot 6H(2)O has been developed for a well-known important natural product, celastrol, resulting in a series of derivatives for further biological evaluation. The catalyst loading was reduced to 5 mol %, the reaction proceeds at ambient temperature and reaction time is only 3 h. The product yields range from 20% to 99%. A reaction mechanism is also proposed, based on our experiment results.

引用

页数：14

共 32 条

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