Journal
JOURNAL OF ORGANIC CHEMISTRY
Volume 82, Issue 18, Pages 9837-9843Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.joc.7b01339
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Funding
- National Natural Science Foundation of China [21576296, 21676302]
- China Postdoctoral Science Foundation [2017M610504]
- Natural Science Foundation of Hunan Province [2017B3401]
- Central South University
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A practical and straightforward synthetic route through a Selectfluor-triggered tandem cyclization of o-hydroxyarylenaminone was developed to construct a variety of difluorinated 2-amino-substituted chromanones. This novel protocol features mild reaction conditions, operational simplicity, and broad substrate scope. The enamine moiety in o-hydroxyarylenaminone played dual roles to enable high efficiency in the difluorination and intrarnolecular cyclization, leading to the accomplishment of a new class of difluorinated 2-amino-substituted chromanones for pharmaceutical studies.
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