Rh(III)-Catalyzed C–H Activation/Cyclization of Indoles and Pyrroles: Divergent Synthesis of Heterocycles
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https://figshare.com/articles/dataset/Rh_III_Catalyzed_C_H_Activation_Cyclization_of_Indoles_and_Pyrroles_Divergent_Synthesis_of_Heterocycles/2273026
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资源简介：
We
report herein a new strategy of the Rh(III)-catalyzed C–H
activation/cyclization of indoles and pyrroles, for the divergent
synthesis of privileged heterocycles. A simple derivation of indoles
and pyrroles to N-carboxamides with oxidative bidentate
directing group could enable rhodacycle formation and late-stage redox-neutral
cyclization with alkynes, alkenes and diazo compounds, for access
to five- and six-membered fused heterocycles, such as pyrimido[1,6-a]indol-1(2H)-one, 3,4-dihydropyrimido[1,6-a]indol-1(2H)-one, and 1H-imidazo[1,5-a]indol-3(2H)-ones.
Kinetic isotope effect study was conducted, and a plausible mechanism
was proposed. Furthermore, this protocol was applied to concise synthesis
of 5-HT3 receptor antagonist in gram-scale.
创建时间：
2016-02-17
