期刊
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
卷 140, 期 35, 页码 10970-10974出版社
AMER CHEMICAL SOC
DOI: 10.1021/jacs.8b07597
关键词
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资金
- NSFC [21602160, 21772148]
- Fundamental Research Funds for the Central Universities [2042018kf0017]
- NSF under the CCI Center for Selective C-H Functionalization (CCHF) [CHE-1700982]
- National Program for 1000 Young Talents of China, Wuhan University
- Caltech
Herein we describe a general, mild and scalable method for deuterium incorporation by potassium methoxide/hexamethyldisilane-mediated dehalogenation of arylhalides. With CD3CN as a deuterium source, a wide array of heteroarenes prevalent in pharmaceuticals and bearing diverse functional groups are labeled with excellent deuterium incorporation (>60 examples). The ipso-selectivity of this method provides precise access to libraries of deuterated indoles and quinolines. The synthetic utility of our method has been demonstrated by the incorporation of deuterium into complex natural and drug-like compounds.
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