期刊
SYNLETT
卷 33, 期 4, 页码 346-350出版社
GEORG THIEME VERLAG KG
DOI: 10.1055/a-1495-6994
关键词
C-H bond activation; arylation; ruthenium catalysis; hetarenes; aryl halides
资金
- DFG [SPP1807]
- Janssen Pharmaceutica
- DFG (Gottfried-Wilhelm-Leibniz award)
A triazole-directed direct C-H arylation of arenes with electron-deficient aryl halides or pyrimidyl chloride was achieved through ruthenium catalysis. This strategy provides a simple and environmentally friendly access to highly functionalized hetarenes, avoiding the use of strong organometallic bases. Detailed studies revealed a significant impact of the phosphine ligand, enabling the reaction to exhibit excellent levels of chemo- and position selectivity.
A triazole-directed direct C-H arylation of arenes with electron-deficient aryl halides or a synthetically useful pyrimidyl chloride was achieved through ruthenium catalysis. Our novel strategy provides operationally simple and environmentally benign access to highly functionalized hetarenes, avoiding the use of strong organometallic bases. Detailed studies revealed a significant effect of the phosphine ligand, thereby permitting the reaction to occur with excellent levels of chemo- and position selectivity.
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