期刊
CHEMICAL SCIENCE
卷 10, 期 45, 页码 10556-10561出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c9sc03710a
关键词
-
资金
- Novartis
- NSF [GOALI 1566212]
A 1 : 1 Pd : ligand complex, [t-BuXPhos(Pd-pi-cinnamyl)]OTf, has been identified as a highly robust pre-catalyst for amination reactions leading to diarylamines, where loadings of metal are typically at 1000 ppm Pd, run in water at temperatures between rt and 45 degrees C. The protocol is exceptionally simple, is readily scaled, and compares very favorably vs. traditional amination conditions. It has also been shown to successfully lead to key intermediates associated with several physiologically active compounds.
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