Abstract
In this paper, a novel series of 2-aminofuro(2,3-d)yrimidin-4(3H)-one derivatives were prepared via aza-Wittig reaction of iminophosphorane 3 with aromatic isocyanate and subsequent reaction with various amine under mild condition in 78%~90% yields. The structures of these compounds were confirmed by mass spectral data, 1 H NMR, IR and elemental analysis. Compound 5c was further analyzed by single crystal X-ray diffraction. The in vitro antitumor activities of com- pounds 5 were analyzed with 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazoliumbromide (MTT) standard method, and compound 5f showed the best inhibition activities against A459 with IC50 18.4 μmol/L. Keywords furo(2,3-d)pyrimidin-4(3H)-one; synthesis; antitumor activity 稠合嘧啶酮衍生物具有丰富的和多样性的化学性
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