Journal
JOURNAL OF ORGANIC CHEMISTRY
Volume 82, Issue 16, Pages 8703-8709Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.joc.7b00732
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Funding
- Shandong Provincial Natural Science Foundation [JQ201604]
- General Project [ZR2016BM07]
- Qingdao Special Research Foundation of Science and Technology [16-6-2-29 nsh]
- Talents of High Level Scientific Research Foundation of Qingdao Agricultural University [6631112323, 6631115 015, 6631110309]
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The first transition-metal free and regioselective C(sp(3))-H arylation of 2-alkylazaarenes with nitroarenes has been achieved via t-BuOK-mediated dehydrogenative C(sp(3))-C(sp(2)) coupling. This reaction provides an efficient access to the biologically important and synthetically useful 2-benzyl-substituted azaarenes under mild conditions without the need of prefunctionalization of 2-alkylazaarenes or using the specialized arylating agents.
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