Journal
ORGANIC LETTERS
Volume 18, Issue 20, Pages 5376-5379Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.6b02755
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Funding
- National Natural Science Foundation of China [81620108027, 21632008, 21602234, 81220108025]
- Major Project of Chinese National Programs for Fundamental Research and Development [2015CB910304]
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In this study we developed a method for the pyridine-directed, rhodium-catalyzed, site-selective C-H alkylation and arylation of pyridones using commercially available trifluoroborate reagents. This simple and versatile transformation proceeded smoothly under relatively mild conditions with perfect site selectivity. The coupling groups in the boron reagents can be extended to primary alkyl, benzyl, and cycloalkyl. Moreover, direct C-H arylation products could also be obtained under similar conditions.
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