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Palladium-Catalyzed Intramolecular C(sp2)-H Amidination by Isonitrile Insertion Provides Direct Access to 4-Aminoquinazolines from N-Arylamidines

Yong Wang, Honggen Wang, Jiangling Peng and Qiang Zhu*

*State Key Laboratory of Respiratory Disease, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, 190 Kaiyuan Avenue, Guangzhou 510530, China, Email:

Y. Wang, H. Wang, J. Peng, Q. Zhu, Org. Lett., 2011, 13, 4596-4599.

DOI: 10.1021/ol201807n


An efficient method enables a synthesis of 4-amino-2-aryl(alkyl)quinazolines from readily available N-arylamidines and isonitriles via palladium-catalyzed intramolecular aryl C-H amidination by isonitrile insertion.

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Key Words

quinazolines, oxygen

ID: J54-Y2011-2450