Journal
CHEMICAL COMMUNICATIONS
Volume 54, Issue 14, Pages 1746-1749Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/c7cc09308j
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Funding
- National Key Research and Development Program of China [2016YFA0602900]
- National Natural Science Foundation of China [21490572, 21420102003]
- Pearl River S&T Nova Program of Guangzhou [201610010160]
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The first example of the palladium-catalyzed primary amine-directed C(sp(2))-H alkynylation of biaryl-2-amines has been developed by using (bromoethynyl) triisopropylsilane as an alkynylating reagent. This protocol exhibits a broad substrate scope, excellent regioselectivity and gram-scale synthesis. Significantly, the versatility of this straightforward method was further demonstrated by controlled mono-and di-alkynylation.
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