4-硫胸苷的合成新方法
New Method for the Synthesis of 4-Thiothymidine
DOI: 10.12677/SSC.2015.33011, PDF, HTML, XML,  被引量 下载: 2,755  浏览: 8,491 
作者: 闫德峰*, 赫玲爽*, 马克东*, 张晓辉*, 李德鹏*:大连大学环境与化学工程学院,辽宁 大连
关键词: 4-硫胸苷Lawesson试剂合成抗肿瘤活性4-Thiothymidine Lawesson Reagent Synthesis Antitumor Activity
摘要: 4-硫胸苷/UVA(长波黑斑效应紫外线)辅助疗法为癌症治疗提供了新的途径,通过对胸苷进行修饰,得到对近紫外光敏感的药物,从而在紫外光的协同作用下达到治疗肿瘤细胞的作用。为了得到新型具有光学性质的4-硫胸苷类药物,传统使用三唑法和P2S5法,而本文采用了新试剂——Lawesson试剂,极大的缩短了反应时间,提高了产率,并用1H-NMR及13C-NMR表征了产物结构。
Abstract: 4-Thiothymidine combined with UVA (light shading effect with long-wave ultraviolet) as a potentially novel therapy for cancer provides a new way, UVA-sensitive 4-thiothymidine was obtained through the study of the modification of thiothymidine at 4-position, and reached the role of treatment of tumor cells under the synergy of UVA. In order to obtain 4-Thiothymidine drugs with new optical properties, triazole and P2S5 are used in previously reported methods. In this study, Lawesson reagent was adopted to prepare 4-thiothymidine. Under the optimized conditions, the reaction time was significantly reduced and the yield increased. The structure of the product was characterized by 1H-NMR and 13C-NMR.
文章引用:闫德峰, 赫玲爽, 马克东, 张晓辉, 李德鹏. 4-硫胸苷的合成新方法[J]. 合成化学研究, 2015, 3(3): 70-73. http://dx.doi.org/10.12677/SSC.2015.33011

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