Journal
JOURNAL OF ORGANIC CHEMISTRY
Volume 76, Issue 15, Pages 6362-6366Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jo2007362
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Funding
- National Science Foundation of China [21072190]
- National Basic Research Program of China (973 Program) [2011CB504004, 2010CB945500]
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An efficient synthesis of quinazolin-4(3H)-ones from N-arylamidines, through palladium-catalyzed intramolecular C(sp(2))-H carboxamidation, has been developed. The reaction, carried out in the presence of 1.0 equiv of CuO as oxidant under atmospheric pressure of CO, provides diversified 2-aryl(alkyl)-quinazolin-4(3H)-ones in reasonable to good yields from N-arylamidines, which are readily derived from anilines and nitriles. Compared with existing approaches to quinazolin-4(3H)-ones, the current strategy features atom-economy and step-efficiency.
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