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Na2S2O3 Catalyzed Three–component Synthesis and Anti–bacterial Activity of 3-methyl-4-(hetero)arylmethylene isoxazole-5(4H)-ones

Yongchang Bi,Jingjun Wang,Xingyu Bian,Mingyue Chen,Guangyuan Zhu,Yumin Zhang,Qiang Gu

An efficient and green method for synthesizing 3-methyl-4-(hetero) arylmethylene isoxazole-5(4 H )-ones was developed using a recyclable and environmental–friendly catalyst, Na 2 S 2 O 3 , and 16 target compounds were successfully synthesized under the obtained optimal reaction condition. Using rifampicin as a positive control, the antibacterial activity of all synthesized compounds was tested by micro dilution method, among them, 3-methyl-4-[(2,4-dimethoxyphenyl) methylene]-isoxazole-5-one ( 4 m ) presented wonderful antimicrobial activity, which may contribute to the development of anti-tuberculosis drugs. Graphical