4.6 Article

p-TsOH-mediated synthesis of substituted 2,4-diaryl-3-sulfonylquinolines from functionalized 2-aminobenzophenones and aromatic β-ketosulfones under microwave irradiation

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ORGANIC & BIOMOLECULAR CHEMISTRY
卷 18, 期 2, 页码 305-315

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ROYAL SOC CHEMISTRY
DOI: 10.1039/c9ob02445j

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  1. Academia Sinica [AS-SUMMIT-108]
  2. Ministry of Science and Technology [MOST 108-3114Y-001-002]

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This study describes an efficient protocol for the preparation of substituted 2,4-diaryl-3-sulfonylquinolines from functionalized 2-aminobenzophenones and aromatic beta-ketosulfones by using p-toluenesulfonic acid monohydrate under microwave irradiation. In this atom-economical synthetic route, a series of pharmaceutically active 3-arylsulfonylquinolines with good functional group tolerance are prepared in good to excellent yields. Some structures are confirmed by single-crystal X-ray diffraction analysis.

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