巯基化叶酸的制备和表征

Synthesis and Characterization of Thiolated Folic Acid

通过对基团的保护和脱保护以及酯化反应,合成了目标产物叶酸的衍生物。首先,用三苯甲基对巯基乙醇的巯基进行保护,保护后的巯基乙醇在催化剂作用下与叶酸发生酯化反应,酯化产物在三氟乙酸(TFA)和三乙基硅烷(TES)作用下脱去三苯甲基。通过红外光谱、紫外可见光谱、元素分析、荧光分光光度计和核磁对产物进行表征。结果表明,巯基成功被保护和脱保护,保护后的巯基乙醇与叶酸的羧基发生了反应,叶酸衍生物具有荧光性能,且在靶向肿瘤诊断治疗方面具有潜在的应用价值。

Folic acid derivatives was synthesized by protection and deprotection of the groups and esterification.To protect the mercapto group in mercaptoethanol,the Trt group was the optimal choice.Folic acid modified by the protection was synthesized through catalyst,then the products was deprotected by TFA and TES.Been characterized by IR,UV-visible spectroscopy,elemental analysis,fluorescence spectrophotometer,and 1H-NMR,the results showed that the-COOH of folic acid and the-SH of mercaptoethanol reacted successfully.The product had fluorescent properties,and might have potential application value in folic acid targeted cancer diagnosis and treatment areas.