期刊
JOURNAL OF ORGANIC CHEMISTRY
卷 85, 期 16, 页码 10902-10912出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.joc.0c01494
关键词
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资金
- JSPS KAKENHI [15H04634, 17K08214]
- Hamamatsu Foundation for Science and Technology Promotion
- Research Foundation for Pharmaceutical Sciences, University of Shizuoka
- Japan Agency for Medical Research and Development (AMED)
- Grants-in-Aid for Scientific Research [17K08214, 15H04634] Funding Source: KAKEN
A palladium-dihydroxyterphenylphosphine (DHTP) catalyst was successfully applied to the direct C3-arylation of N-unsubstituted indoles with aryl chlorides, triflates, and nonaflates. This catalyst showed C3-selectivity, whereas catalysts with other structurally related ligands exhibited N1-selectivity. Complex formation between the lithium salts of the ligand and the indole is assumed to accelerate the arylation at the C3 position. Reactions using 3-alkylindoles afforded 3,3-disubstituted indolenines, which can be further converted to the corresponding indoline derivatives.
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