4-硫胸苷的合成新方法
New Method for the Synthesis of 4-Thiothymidine

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 (2015) 4-硫胸苷的合成新方法。 合成化学研究, 3, 70-73. doi: 10.12677/SSC.2015.33011

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