摘要
报道应用aza-Wittig反应,采用易得的原料,在温和的条件下,以78%~90%的产率有效的合成了新型2-氨基-呋喃并[3,2-d]嘧啶-4(3H)-酮衍生物5,其结构经IR,1H NMR,MS和元素分析确认.为进一步得到结构确认,化合物5c经X射线衍射分析证实.运用噻唑蓝(MTT)标准法对化合物5进行了体外抗肿瘤活性的测定,其中5f对肺癌细胞A459的IC50值为18.4μmol/L,显示出潜在良好的抗肿瘤活性.
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 IC5018.4 μmol/L.
出处
《有机化学》
SCIE
CAS
CSCD
北大核心
2012年第8期1468-1472,共5页
Chinese Journal of Organic Chemistry
基金
湖北省科技厅自然科学基金(No.2011CDB08301)
湖北省教育厅研究(Nos.D20092406
Q20102110)
湖北医药学院优秀中青年科技创新团队研究(Nos.2011CXX03
2009QDJ15)资助项目~~