期刊
ORGANIC LETTERS
卷 17, 期 15, 页码 3738-3741出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.5b01710
关键词
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资金
- Indiana University-Purdue University Indianapolis
- NSF [CHE-1350541]
- Robert A. Welch Foundation, USA [D-1361]
- NSFC [21332005]
- Jiangsu Innovation Programs (P. R. China)
The transition-metal-catalyzed direct C-H bond fluorination is an attractive synthetic tool toward the preparation of organofluorines. While many methods exist for the direct sp(3) C-H functionalization, site-selective fluorination of unactivated sp(3) carbons remains a challenge. Direct, highly site-selective and diastereoselective fluorination of aliphatic amides via a palladium-catalyzed bidentate ligand-directed C-H bond functionalization process on unactivated sp3 carbons is reported. With this approach, a wide variety of beta-fluorinated amino acid derivatives and aliphatic amides, important motifs in medicinal and agricultural chemistry, were prepared with palladium acetate as the catalyst and Selectfluor as the fluorine source.
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