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The aza-Wittig reactions of iminophosphorane  3  with aromatic isocyanates generated carbodiimides  4 , which were reacted with alkylamines under mild conditions to give a series of 2-(alkylamino)-5,6-dimethylthieno[2,3- d ]pyrimidin-4(3 H )-ones  6  and  8  in satisfactory yield. Their structures were confirmed by  1 H NMR, EI-MS, IR and elementary analysis, and compound  8c  was further analyzed by single-crystal X-ray diffraction. The preliminary bioassays indicated that these compounds showed excellent fungicidal activities against six kinds of fungi.

A facile synthesis and fungicidal activities of 2-(alkylamino)-5,6-dimethylthieno[2,3-d]pyrimidin-4(3H)-ones