Journal
TETRAHEDRON
Volume 67, Issue 32, Pages 5776-5783Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tet.2011.05.134
Keywords
Cross-coupling; Heterogeneous catalysis; Homogeneous catalysis; Palladium; Quinolin-4(1H)-ones
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Funding
- Siena Biotech S.p.A., Siena (Italy)
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A practical and general synthesis of 1,3,6-trisubstituted quinolin-4(1H)-ones starting from 1-alkyl-6-bromo-3-iodoquinolin-4(1H)-one is described, based on regioselective sequential palladium-catalyzed cross-coupling reactions, namely Suzuki-Miyaura, Sonogashira and aminocarbonylation reactions, under microwave irradiation. Good substrate generality, ease of execution and practicability make this method exploitable for the generation of libraries of chemically diverse 4-quinolones. (C) 2011 Elsevier Ltd. All rights reserved.
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