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. 2016 Sep 12;18(9):604-10.
doi: 10.1021/acscombsci.6b00082. Epub 2016 Aug 24.

Facile Synthesis of Azaarene-Substituted Hydroxycoumarins Possessing High Biological Activities via Three-Component C(sp(3))-H Functionalization

Haoxun Dong  1 , Lubin Xu  1 , Shuai-Shuai Li  1 , Liang Wang  1 , Chang-Lun Shao  2 , Jian Xiao  1
Affiliations

Facile Synthesis of Azaarene-Substituted Hydroxycoumarins Possessing High Biological Activities via Three-Component C(sp(3))-H Functionalization

Haoxun Dong et al. ACS Comb Sci. .

Abstract

An unprecedented three-component C(sp(3))-H functionalization of 2-alkylazaarenes with aryl aldehydes and 4-hydroxycoumarins was realized, providing azaarene-substituted 3-benzyl-4-hydroxycoumarins in good to excellent yields. These new target compounds displayed broad-spectrum antibacterial activities, providing a new type of antibacterial skeleton.

Keywords: 2-alkylazaarenes; 3-benzyl-4-hydroxycoumarins; 4-hydroxycoumarins; C(sp3)−H functionalization; aryl aldehydes; biological activities; three-component.

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