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A Convenient Synthesis and Biological Activity of Novel Pyrido[4,3‐ d ]pyrimidin‐4(3 H )‐ones
Author(s) -
Ren Qingyun,
Xia ShiYan,
Gu Yucheng,
Li Baoju,
He Hongwu
Publication year - 2015
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.2119
Subject(s) - chemistry , annulation , aryl , isocyanate , antifungal , wittig reaction , nuclear magnetic resonance spectroscopy , bioassay , tandem , combinatorial chemistry , elemental analysis , spectroscopy , stereochemistry , organic chemistry , medicinal chemistry , polyurethane , medicine , alkyl , materials science , physics , composite material , dermatology , quantum mechanics , biology , genetics , catalysis
Fifteen novel 2‐alkylamino‐3‐aryl‐8‐cyano‐5‐methyl‐7‐(methylthio)‐pyrido[4,3‐ d ]pyrimidin‐4(3 H )‐ones 6a , 6b , 6c , 6d , 6e , 6f , 6g , 6h , 6i , 6j , 6k , 6l , 6m , 6n , 6o were designed and have been successfully synthesized via tandem aza‐Wittig and annulation reactions with the corresponding iminophosphoranes 4 , aryl isocyanate, and amines in good yields. Their structures were clearly verified by IR spectroscopy, 1 H‐NMR spectroscopy, EI‐MS, and elemental analysis, and in the case of compound 6i , further analyzed by single‐crystal X‐ray diffraction. The preliminary results of an in vivo bioassay showed that some compounds display moderate antifungal activity.