Copper-Mediated monochlorination of anilines and nitrogen-containing heterocycles |
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| Authors: | Xue-Yan Yang Hong-Yi Zhao Shuai Mao |
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| Institution: | Department of Medicinal Chemistry, School of Pharmacy, Xi'an Jiaotong University, Xi'an, P. R. China |
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| Abstract: | A simple and selective copper(II) chloride-mediated monochlorination of anilines and nitrogen-containing heterocycles has been developed. Stirring a mixture of aniline, copper(II) chloride, lithium chloride in EtOH under reflux condition produced 4-chloroaniline with high yield. Eighteen substrates including substituted anilines, N-substituted anilines, N,N-disubstituted anilines, 5-nitroindole and carbazole were all reactive and afforded desired products in moderate to excellent yields (52%–98%). |
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| Keywords: | Aniline chlorination copper chloride lithium chloride |
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