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, 1H 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 mmol/L.
Hu Yanggen
,
Gao Haitao
,
Wang Gang
,
Wang Yan
,
Qu Yongnian
,
Xu Jing
. Synthesis and Antitumor Activity of Some 2-Amino-furo[2,3-d]- yrimidin-4(3H)-one Derivatives[J]. Chinese Journal of Organic Chemistry, 2012
, 32(08)
: 1468
-1472
.
DOI: 10.6023/cjoc201203003
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