Iron-catalyzed [4 + 2] annulation of amidines with α,β-unsaturated ketoxime acetates toward 2,4,6-trisubstituted pyrimidines

    • Qinghuan Wua, Luchao Lia, Binyan Xua, Jie Suna, Dong Jib, Yuguang Lib, Lei Shenb, Zheng Fanga, Jindian Duana, Beining Chenc, Kai Guoa
    • aCollege of Biotechnology and Pharmaceutical Engineering, State Key Laboratory of Materials-Oriented Chemical Engineering, Nanjing Tech University, Nanjing, 211816, China
    • bInstitute of Nanjing Advanced Biomaterials & Processing Equipment, Nanjing, 211299, China
    • cDepartment of Chemistry, University of Sheffield, Sheffield, S3 7HF, UK

    An iron-catalyzed [4 + 2] annulation of amidines with α,β-unsaturated ketoxime acetates is described. This strategy employs amidines as CN units and provides a new protocol for the construction of 2,4,6-trisubstituted pyrimidines under batch and continuous flow conditions in moderate to good yields, exhibiting good functional group tolerance, scalability and operational simplicity.

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