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Copper-Mediated Cyclization of o -Hydroxyaryl Enaminones with 3-Indoleacetic Acids toward the Synthesis of 3-Indolmethyl-Chromones.

Kangmei WenYinyan LiQiwen GaoJiewen ChenJie YangXiaodong Tang
Published in: The Journal of organic chemistry (2022)
Here, we describe a copper-mediated tandem decarboxylative coupling/annulation protocol of o -hydroxyaryl enaminones with 3-indoleacetic acids. A series of 3-indolmethyl-chromones were afforded in up to 97% yield. A one-pot method for 3-indolmethyl-chromones from o -hydroxy acetophenones, N , N -dimethylformamide dimethyl acetal, and 3-indoleacetic acids was also developed. Derivatization of the products was conducted to provide various indolmethyl-substituted pyrimidines. Moreover, a biological evaluation revealed that some compounds had anti-influenza viral activities.
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