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Gold-Catalyzed Three-Component Tandem Process: An Efficient and Facile Assembly of Complex Butenolides from Alkynes, Amines, and Glyoxylic Acid
Qiang Zhang
†‡, Ming Cheng
†‡, Xiaoyu Hu
†‡, Bo-Gang Li
† and Jian-Xin Ji
*†Chengdu Institute of Biology, Chinese Academy of Sciences, Chengdu 610041, People’s Republic of China, and Graduate School of the Chinese Academy of Sciences, Beijing 100039, People’s Republic of China
J. Am. Chem. Soc., 2010, 132 (21), pp 7256–7257
DOI: 10.1021/ja101804p
Publication Date (Web): May 10, 2010
Copyright © 2010 American Chemical Society
jijx@cib.ac.cn, †
Chengdu Institute of Biology.
, ‡
Graduate School of the Chinese Academy of Sciences.
Abstract
An efficient and facile gold-catalyzed three-component tandem process for the assembly of two types of highly functionalized butenolides has been developed. In this reaction system, more than four chemical bonds are formed by a single gold catalyst. The present tandem protocol includes a direct coupling of alkynes, amines, and glyoxylic acid and subsequent exclusively endo-selective cycloisomerization of alkynoic acids along with intermolecular electrophilic trapping; it utilizes three simple and commercially available starting materials to assemble architecturally complex and appealing butenolide scaffolds bearing other reactive sites for further manipulation.
详细资料
- 文献种类: Journal Article
- 期刊名称: Journal of the American Chemical Society
- 期刊缩写: J. Am. Chem. Soc.
- 期卷页: 2010年 第132卷 第21期 7256-7257页
- ISBN: 0002-7863
唐唐 的文献笔记
|
金催化多组分反应研究取得进展
在新药设计和研发过程中，随着功能基因组学、蛋白质组学和结构生物学等学科的迅速发展， 越来越多的新靶点不断地被发现和阐明。同时，高通量筛选技术的长足进步为大规模的化合物筛选提供了快速方便的途径。这些进步给化学家提出了一个新的挑战， 就是如何快速大量地提供具有结构多样性和复杂性的新化学实体，用于通过筛选来发现活性化合物，这已成为制约现代化学药物发现研究的技术瓶颈之一。
最近，中国科学院成都生物研究所天然产物研究中心分子结构多样性构建和药物化学实验室博 士研究生张强、成明、胡晓玉在导师姬建新研究员和李伯刚研究员的启发引导下，发展了金催化的炔—胺—乙醛酸（Alkyne—Amine— Glyoxylic acid）三组分串联反应过程，快速高效地构建α，β-不饱和-γ-丁内酯类化合物。该研究成果发表在J. Am. Chem. Soc. 2010, 132, 7256-7257上。
γ-丁内酯结构片段大量存在于具有广泛生物活性的天然产物中，该结构单元也是某些药物的 重要砌块。该反应体系实现了金催化的炔—胺—乙醛酸三组分的“一锅法”反应，将简单易得，种类多样的化学原料组装成为可进行下一步反应的底物，然后完成分 子内环合反应和进一步转化，从而简洁高效地构建了结构较为复杂和多样两类γ-丁内酯类化合物。
目前，进一步的研究工作正在进行中。 |
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Gold-Catalyzed Three-Component Tandem Process: An Efficient and Facile Assembly of Complex Butenolides from Alkynes, Amines, and Glyoxylic Acid 
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