國家衛生研究院 NHRI:Item 3990099045/10456
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    题名: Diversity-oriented synthesis of coumarin-linked benzimidazoles via a one-pot, three-step, intramolecular knoevenagel cyclization
    作者: Yao, PHE;Kumar, S;Liu, YL;Fang, CP;Liu, CC;Sun, CM
    贡献者: Center for Neuropsychiatric Research
    摘要: Diversity-oriented synthesis of coumarin-linked benzimidazoles from N-(2-aminophenyl)-2-cyanoacetamide was achieved via a one-pot, three-step sequential reaction in excellent yields. In situ intramolecular cyclization of the cyanoacetamide afforded benzimidazoles which subsequently underwent a Knoevenagel condensation of the 2-cyanomethylbenzimidazoles with salicylaldehydes promoted by triethylamine to reach the target compounds. An important intermediate, 2-(2-imino-2H-chromen-3-yl)-1H-benzimidazole was characterized by X-ray analysis and further hydrolyzed to 2-(coumarin-3-yl)benzimidazole in acidic condition. Among the synthesized compounds, some were found to be promising inhibitors of porcine kidney d-amino acid oxidase (pkDAO).
    日期: 2017-02-14
    關聯: ACS Combinatorial Science. 2017 Feb 14;19(4):271-275.
    Link to: http://dx.doi.org/10.1021/acscombsci.7b00004
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000399061000008
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=85017501033
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