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Efficient Construction of Drug-like Bispirocyclic Scaffolds Via Organocatalytic Cycloadditions of α-Imino γ-Lactones and Alkylidene Pyrazolones
Published on: February 7, 2019
Synthesis of Indole-Fused Oxepane through (4 + 3) Cycloadditions of Indolyldimethanols with Pyrazolones
1School of Chemistry and Chemical Engineering/State Key Laboratory Incubation Base for Green Processing of Chemical Engineering, Shihezi University, Shihezi, Xinjiang832003, China.
Abstract:
An efficient phosphoric acid-catalyzed cycloaddition reaction between pyrazolones and 2-indolyldimethanols for the construction of indole-fused seven-membered oxepane skeletons was developed. This protocol featured excellent functional group tolerance, broad substrate generality, and high reaction yields. Moreover, the scalable gram-scale synthesis and facile product derivatization further demonstrated its synthetic practicability. This work provided a reliable strategy for the assembly of complex oxepane heterocyclic frameworks.
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