摘要
应用5,6,7,8-四氢苯并噻吩膦亚胺(2)与烷基异氰酸酯的氮杂Wittig反应生成碳二亚胺2,在不同的条件下,2分别与不同的亲核试剂反应,有效地合成了不同取代的新型稠合噻吩并[2,3-d]嘧啶-4(3H)-酮衍生物.所得化合物的结构由1H NMR,IR,MS和元素分析所确证.初步的体外抗肿瘤活性测试,结果显示目标化合物具有抑制肿瘤细胞的生长,其中5d对口腔肿瘤细胞KB2IC50值为19.0μmol/L,表现出潜在的抗肿瘤活性.
The aza-Wittig reaction of iminophosphorane 2 with alkyl isocyanates gave carbodiimides 3, which were allowed to react with various nucleophilic reagents under mild condition in satisfactory yields to prepare a novel series of 5,6,7,8-tetrahydrobenzothieno[2,3-d]pyrimidin-4（3H）-one derivatives. The structures of these compounds were confirmed by IH NMR, IR, MS and elemental analysis. The in vitro antitumor activities of compounds were analyzed with 3-（4,5-dimethylthiazol-2-yl）-2,5-diphenyltetrazo-liumbromide （MTT） standard method, 5d stood out as the most potent showing an IC50 of 19.0 μmol/L against human tumor cell lines （KB）.
出处
《有机化学》
SCIE
CAS
CSCD
北大核心
2015年第5期1075-1080,共6页
Chinese Journal of Organic Chemistry
基金
湖北自然科学基金(No.2011CDC006)
湖北省2011协同创新中心基金(No.2011JH-2014CXTT07)
湖北医药学院优秀中青年科技创新团队研究(Nos.2011CXX03
2009QDJ15
2014XKJSXJ06)资助项目~~
