Journal
GREEN CHEMISTRY
Volume 22, Issue 21, Pages 7506-7512Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/d0gc02134b
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Funding
- National Natural Science Foundation of China [21971165, 21921002]
- National Key R&D Program of China [2018YFA0903500]
- 1000-Youth Talents Program [YJ201702]
- Fundamental Research Funds for the Central Universities
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Herein, a transition-metal-free multicomponent cascade reaction of readily available alpha-halogenated ketones, ortho-aminophenols, and aldehydes using a novel dipeptide-based phosphonium salt catalyst was developed for the efficient construction of various 2H-1,4-benzoxazine derivatives with excellent functional-group tolerance. The method represents an unprecedented approach for trapping active 1,5-bifunctional intermediates with alpha-halogenated ketones to access biologically important benzoxazine scaffolds bearing two stereogenic centers with excellent asymmetric induction.
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