Synthesis and and Antitumor Activity of Some 2-Amino-furo[2,3-d]yrimidin-4(3H)-one Derivatives

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%similar to 90% yields. The structures of these compounds were confirmed by mass spectral data, H-1 NMR, IR and elemental analysis. Compound 5c was further analyzed by single crystal X-ray diffraction. The in vitro antitumor activities of compounds 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 mu mol/L.