A mild and efficient synthesis of 4-quinolones and quinolone heterocycles |
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Authors: | Zewge Daniel Chen Cheng-Yi Deer Curtis Dormer Peter G Hughes Dave L |
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Institution: | Department of Process Research, Merck Research Laboratories, P.O. Box 2000, Rahway, New Jersey 07065, USA. daniel_zewge@merck.com |
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Abstract: | The cycloacylation of aniline derivatives to 4-quinolones in the presence of Eaton's reagent is described. This high-yielding methodology is applicable to a wide variety of functionalized anilines and requires milder conditions than those traditionally employed. This cyclization protocol is used to prepare a host of heterocycles and bis-quinolones and is characterized by relatively low reaction temperature and ease of product isolation. |
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