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An Efficient One-Pot Synthesis of Substituted 2-Aminothiophenes via Three-Component Gewald Reaction Catalyzed by L-Proline

Tao Wang, Xian-Gui Huang, Jia Liu, Bo Li, Jin-Jin Wu, Kai-Xian Chen, Wei-Liang Zhu, Xiao-Yong Xu*, Bu-Bing Zeng*

*Shanghai Key Laboratory of Chemical Biology, Shanghai 200237, P. R. of China, Email:,

T. Wang, X.-G. Huang, J. Liu, B. Li, J.-J. Wu, K.-X. Chen, W.-L. Zhu, X.-Y. Xu, B.-B. Zeng, Synlett, 2010, 1351-1354.

DOI: 10.1055/s-0029-1219917

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An efficient one-pot procedure allows the synthesis of various functionalized 2-aminothiophene scaffolds catalyzed by L-proline in high yields under mild conditions. Low catalyst loading, simple procedure, and high yields are the important attributes of this methodology.

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Key Words

Gewald Reaction, 2-aminothiophenes, thiophenes, one-pot, organocatalysis, multicomponent reactions, Knoevenagel reaction

ID: J60-Y2010-1570