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Copper-catalyzed Direct 2-Arylation of Benzoxazoles and Benzoimidazoles with Aryl Bromides and Cytotoxicity of Products.

ABSTRACT: An efficient copper-catalyzed direct 2-arylation of benzoxazoles and benzoimidazoles with aryl bromides is presented. The CuI/PPh₃-based catalyst promotes the installation of various aryl and heteroaryl groups through a C-H activation process in good to excellent yields. The cytotoxicity of obtained 2-aryl benzoxazoles (benzoimidazoles) was also evaluated and 1-methyl-2-(naphthalen-1-yl)benzoimidazole showed potential cytotoxicity.

SUBMITTER: Jia NN

PROVIDER: S-EPMC5335610 | biostudies-literature | 2017 Mar

REPOSITORIES: biostudies-literature

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Copper-catalyzed Direct 2-Arylation of Benzoxazoles and Benzoimidazoles with Aryl Bromides and Cytotoxicity of Products.

Jia Nan-Nan NN Tian Xin-Chuan XC Qu Xiao-Xia XX Chen Xing-Xiu XX Cao Ya-Nan YN Yao Yun-Xin YX Gao Feng F Zhou Xian-Li XL

Scientific reports 20170303

An efficient copper-catalyzed direct 2-arylation of benzoxazoles and benzoimidazoles with aryl bromides is presented. The CuI/PPh<sub>3</sub>-based catalyst promotes the installation of various aryl and heteroaryl groups through a C-H activation process in good to excellent yields. The cytotoxicity of obtained 2-aryl benzoxazoles (benzoimidazoles) was also evaluated and 1-methyl-2-(naphthalen-1-yl)benzoimidazole showed potential cytotoxicity. ...[more]

PMID: 28256577

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