期刊
JOURNAL OF ORGANIC CHEMISTRY
卷 80, 期 9, 页码 4532-4544出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.joc.5b00378
关键词
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资金
- ANR NeoACAT (JC program)
- region Basse-Normandie
An efficient Method has been developed for direct amide bond synthesis between carboxylic acids and amines via (2-(thiophen-2-ylmethyl)phenyl)boronic acid as a highly active bench-stable catalyst. This catalyst was found to be very effective at room temperature for a large range of substrates with slightly higher temperatures required for challenging ones. This methodology can be applied to aliphatic, alpha-hydroxyl, aromatic, and heteroaromatic acids as well as primary, secondary, heterocyclic, and even functionalized amines. Notably, N-Boc-protected amino acids were successfully coupled in good yields with very little racemization. An example of catalytic dipeptide synthesis is reported.
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