期刊
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
卷 60, 期 3, 页码 1605-1609出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.202011342
关键词
asymmetric synthesis; hydroarylation; nickel; vinyl amides; α -aryl amides
资金
- European Research Council (ERC) [307948]
- Swiss National Science Foundation [SNF 200020_146853]
- Swiss National Science Foundation (SNF) [200020_146853] Funding Source: Swiss National Science Foundation (SNF)
This study presents a nickel-catalyzed asymmetric reductive hydroarylation method for synthesizing enantioenriched alpha-arylbenzamides. By using a BIm ligand, diethoxymethylsilane, and aryl halides, aryl groups can be selectively introduced to the internal position of the olefin, creating a new stereogenic center alpha to the N atom with neutral reagents and mild reaction conditions. This provides a straightforward route to pharmacologically relevant motifs found in anticancer drugs, SARS-CoV PLpro inhibitors, and KCNQ channel openers.
A nickel-catalyzed asymmetric reductive hydroarylation of vinyl amides to produce enantioenriched alpha-arylbenzamides is reported. The use of a chiral bisimidazoline (BIm) ligand, in combination with diethoxymethylsilane and aryl halides, enables the regioselective introduction of aryl groups to the internal position of the olefin, forging a new stereogenic center alpha to the N atom. The use of neutral reagents and mild reaction conditions provides simple access to pharmacologically relevant motifs present in anticancer, SARS-CoV PLpro inhibitors, and KCNQ channel openers.
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