Journal
JOURNAL OF ORGANIC CHEMISTRY
Volume -, Issue -, Pages -Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.joc.2c01334
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Funding
- NSFC [22101074, 21877206, 21772032]
- 111 Project [D17007]
- Excellent Youth Foundation of Henan Scientific Committee [222300420012]
- China Post-doctoral Science Foundation [2019 M660173]
- Natural Science Foundation of Henan Province [202300410233]
- Henan Key Laboratory of Organic Functional Molecules and Drug Innovation
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An efficient and convenient method for the synthesis of indolo[2,1-a]isoquinolines was reported. This reaction involved the Rh(III)-catalyzed double aryl C(sp2)-H bond and N-H activation and annulation, with the presence of Cu(OAc)2 as the oxidant and under heating conditions. Notably, 1,3-diarylurea could serve as a precursor for the generation of two arylamine molecules, diverging from previous studies.
An efficient and convenient Rh(III)-catalyzed double aryl C(sp2)-H bond and N-H activation and annulation reaction is reported for the synthesis of indolo[2,1-a]isoquinolines in the presence of the Cu(OAc)2 oxidant under heating conditions. Distinct from previous works with other arylamine donors, one molecule of 1,3-diarylurea can serve as a precursor of two molecules of arylamine in the reaction with diaryl-substituted alkynes.
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