一锅法合成B-降胆甾-3,5-二烯-α-氨基磷酸酯及细胞活性研究  

One Pot Synthesis of B-norcholesteric-3,5-diene-α-aminophosphate and its Cytotoxicity

作　　者：陈勇 戚彬彬 刘志平 黄燕敏 甘春芳 崔建国 CHEN Yong;QI Binbin;LIU Zhiping;HUANG Yanmin;GAN Chunfang;CUI Jianguo(College of Chemistry and Material Science,Nanning Normal University,Nanning 530001,China)

机构地区：[1]南宁师范大学化学与材料学院,广西南宁530001

出　　处：《化工技术与开发》2022年第1期6-9,共4页Technology & Development of Chemical Industry

基　　金：广西自然科学基金项目(2020GXNSFAA159096);广西创新发展专项项目(AA18242027);广西高等学校高水平创新团队“高效环保新型农药创新团队”。

摘　　要：从胆甾醇(1)出发,通过臭氧氧化、羟醛缩合等反应,合成了B-降-3,5-二羟基胆甾-6-醛(2),然后采用一锅法,与不同结构的伯胺及亚磷酸二乙酯合成了8个结构新颖的B-降胆甾-3,5-二烯-α-氨基磷酸酯(3a~3h)。采用IR、NMR及HR-MS等分析手段进行了结构表征。体外抗肿瘤活性测试结果显示,3a~3h对人体人肝癌细胞(HEPG2)、人鼻咽癌细胞(CNE-2)及宫颈癌细胞株(HeLa)无明显的抑制作用。Started from cholesterol(1),b-norcholestane(2)was synthesized by ozonation and aldol condensation.Then,eight novel B-norcholesteric-3,5-diene-α-aminophosphates(3a~3h)were synthesized with different primary amines and phosphites in one pot.The structures of compounds 3a~3h were characterized by IR,NMR and HRMS.The antitumor activity test in vitro showed that 3a~3h had no obvious inhibitory effect to human hepatoma cell line(HepG2),human nasopharyngeal carcinoma cell line(CNE-2)and human cervical cancer cell lines(Hela).

关 键 词：胆甾醇 氨基磷酸酯 细胞活性 

分 类 号：O629.71[理学—有机化学]