Dahan Wang , Yuhan Yang , Fuhong Xiao , Jinbing Liu , Guojiang Mao , Guo-Jun Deng
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Synthesis of biheteroaryls via 2-methyl quinoline C(sp3)-H functionalization under metal-free conditions
An acetic acid-promoted C(sp3)-H functionalization of 2-methyl quinoline, enaminoesters and elemental sulfur for the synthesis of 3,4,5-trisubstituted isothiazoles under metal-free conditions has been developed. This approach provides viable access to various 5-(quinolin-2-yl)isothiazoles in moderate to good yields with good functional group tolerance. Moreover, the success of the gram-scale reaction gives this reaction a great potential application.
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