3.8 Article

Quick Access to Drug-like Heterocycles: Facile Silver-Catalyzed One-Pot Multicomponent Synthesis of Aminoindolizines

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JOURNAL OF COMBINATORIAL CHEMISTRY
卷 12, 期 5, 页码 696-699

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AMER CHEMICAL SOC
DOI: 10.1021/cc100086h

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  1. Nanyang Technological University [RG50/08]
  2. Ministry of Health, Singapore (NMRC) [H1N1R/001/2009]

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A direct and efficient approach to 1-aminoindolizines through three-component one-pot reaction of heteroaryl aldehydes, secondary amines, and terminal alkynes catalyzed by AgBF4 has been developed. Desired products were obtained in moderate to excellent yields. Similar aminoindolizines products were afforded from trimethylsilyl protected alkyne substrates as well. This methodology provides a rapid access to construct a diversity-oriented library of indolizines.

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