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Published on: November 9, 2019
One-pot synthesis of quinoline-based tetracycles by a tandem three-component reaction
Chao Che1, Jing Xiang, Guo-Xin Wang
1Laboratory of Chemical Genomics, Shenzhen Graduate School, Peking University, Beijing, 100871.
Abstract:
A practical one-pot synthetic strategy for the efficient synthesis of a range of structurally interesting and bioactive quinoline-based tetracycles has been developed. A key step in the synthesis is a tandem three-component reaction of heteroaromatic amine, methyl 2-formylbenzoate and (t)butyl isonitrile, followed by TFA-mediated lactamization via intramolecular aminolysis of an adjacent ester. Results related to a kinase-panel screening for several selected compounds are also discussed in this article.
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