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微波辅助合成7-氮杂吲哚:卤代芳胺与末端炔烃的铁催化环化反应

Microwave-assisted synthesis of 7-azaindoles iron-catalyzed cyclization of an -haloaromatic amine with terminal alkynes.

作者信息

Le Yi, Yang Zhisong, Chen Yumei, Chen Dongmei, Yan Longjia, Wang Zhenchao, Ouyang Guiping

机构信息

State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, State-Local Joint Laboratory for Comprehensive Utilization of Biomass, Center for Research and Development of Fine Chemicals, Guizhou University Guiyang 550025 China.

School of Pharmaceutical Sciences, Guizhou University Guiyang 550025 China

出版信息

RSC Adv. 2019 Dec 2;9(68):39684-39688. doi: 10.1039/c9ra08742g.

DOI:10.1039/c9ra08742g
PMID:35541389
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9076099/
Abstract

An efficient and practical procedure was developed to prepare 7-azaindole, starting from an -haloaromatic amine and corresponding terminal alkynes under microwave irradiation and the scope was demonstrated with a number of examples. The valuable features of this procedure included the iron-catalyzed cyclization, short reaction times and convenient operation. Furthermore, iron catalysis is an interesting alternative to homogeneous catalysis for the synthesis of heterocycles.

摘要

开发了一种高效实用的方法,以卤代芳胺和相应的末端炔烃为原料,在微波辐射下制备7-氮杂吲哚,并通过多个实例展示了其适用范围。该方法的可贵之处包括铁催化环化、反应时间短和操作简便。此外,铁催化是合成杂环化合物时替代均相催化的一种有趣选择。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e42c/9076099/f5d3bc328950/c9ra08742g-s2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e42c/9076099/7df07e1c33a9/c9ra08742g-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e42c/9076099/a3fb602f7651/c9ra08742g-f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e42c/9076099/a71a57eaf2a9/c9ra08742g-s1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e42c/9076099/f5d3bc328950/c9ra08742g-s2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e42c/9076099/7df07e1c33a9/c9ra08742g-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e42c/9076099/a3fb602f7651/c9ra08742g-f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e42c/9076099/a71a57eaf2a9/c9ra08742g-s1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e42c/9076099/f5d3bc328950/c9ra08742g-s2.jpg

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Iron-Catalyzed Cross-Couplings in the Synthesis of Pharmaceuticals: In Pursuit of Sustainability.
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