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Synfacts 2011(10): 1052-1052  
DOI: 10.1055/s-0030-1261101
Synthesis of Heterocycles
© Georg Thieme Verlag Stuttgart ˙ New York

Pd-Catalyzed Synthesis of Quinazolin-4(3H)-ones from N-Aryl Amidines

Contributor(s): Victor Snieckus, Yigang Zhao
B. Ma, Y. Wang, J. Peng, Q. Zhu*
Guangzhou Institutes of Biomedicine and Health, P. R. of China
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Publikationsdatum:
20. September 2011 (online)

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Significance

Reported is a concise synthesis of quinazolin-4(3H)-ones, in which readily available N-aryl amidines in the presence of CO smoothly undergo a Pd-catalyzed intramolecular C-H activation-carboxamidation to afford the quinazolin­one products in moderate to good yields. Notably, 1 atm of CO is sufficient for this process. However, the reaction scope and limitations were not well investigated.