Base-Promoted Metal-/Oxidant-Free Three-Component Tandem Annulation: A Strategy for the Construction of 2,4,5-Trisubstituted Thiazoles via C-N Bond Cleavage of Amidines

被引：15

作者：

Guo, Wei ^{[1
]}

Zhao, Mingming ^{[1
]}

Tan, Wen ^{[1
]}

Zheng, Lvyin ^{[1
]}

Tao, Kailiang ^{[1
]}

Chen, Luyan ^{[1
]}

Wang, Mingfeng ^{[1
]}

Chen, Deliang ^{[1
]}

Fan, Xiaolin ^{[1
]}

机构：

[1] Gannan Normal Univ, Key Lab Organopharmaceut Chem Jiangxi Prov, Ganzhou 341000, Peoples R China

来源：

ASIAN JOURNAL OF ORGANIC CHEMISTRY | 2018年 / 7卷 / 09期

基金：

中国国家自然科学基金;

关键词：

annulation; C-N bond cleavage; heterocycles; multicomponent reactions; thiazoles; FACILE SYNTHESIS; MULTICOMPONENT SYNTHESIS; CATALYZED CYCLIZATION; PYRIMIDINES; DERIVATIVES; 1,3,5-TRIAZINES; METHYLARENES; ACTIVATION; DISCOVERY; MUSCARINE;

D O I：

10.1002/ajoc.201800417

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A base-promoted and metal-/oxidant-free one-pot three-component tandem annulation of amidines, aryl/alkyl isothiocyanates, and -bromoesters/ketones to 2,4,5-trisubstituted thiazoles is described. This operationally simple protocol involves a base-promoted C-N bond cleavage of amidines and features readily available starting materials, excellent functional group tolerance, and high step-economy. It leads to the preparation of 2,4,5-trisubstituted thiazoles efficiently and has potential applications in the field of drug screening and modification.

引用

页码：1893 / 1897

页数：5

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