Direct synthesis of ortho-dihalogenated arylpyrimidines using calcium halides as halogen sources |
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Authors: | Xiaojian Zheng Guifei Li Hongmei Deng |
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Institution: | a Department of Chemistry, Shanghai University, Shanghai 200444, China b Instrumental Analysis and Research Center, Shanghai University, Shanghai 200444, China |
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Abstract: | Pyrimidines and their derivatives have been used as important motifs in materials and medicinal chemistry. In this Letter, a wide variety of ortho-dihalogenated arylpyrimidines were synthesized with high yields and functional-group tolerance using calcium halides as crucial halogenating agents and cupric trifluoroacetate as oxidant in the presence of air. The generated dichlorinated products could be further manipulated by stepwise Suzuki-Miyaura reaction to afford a wide range of ortho-functionalized arylpyrimidines amenable to physical and biological evaluations. |
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Keywords: | Calcium halides C-H activation Cross-coupling Halogenation Nitrogen heterocycles |
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