论文部分内容阅读
核苷类似物因其显著的抗病毒、抗肿瘤活性,已作为化疗药物在临床上得到了广泛应用。核苷类似物的高效绿色合成是有机化学和药物化学领域的重要课题。本文对近年来离子液体介质中的核苷改造进行了综述,主要包括羟基和氨基的保护、糖基的改造、碱基的改造、糖基与碱基的耦合和寡核苷酸的合成。离子液体作为一类物理化学性能“可设计”的绿色软介质材料,应用在核苷的化学合成中,不仅增加了核苷化合物的溶解度,提高了核苷类似物的合成效率,而且避免了有机溶剂产生的毒害。
Nucleoside analogues have been widely used as chemotherapy drugs because of their significant anti-virus and anti-tumor activity. The efficient green synthesis of nucleoside analogues is an important topic in the field of organic chemistry and pharmaceutical chemistry. In this paper, the recent progress in nucleoside conversion in ionic liquids was reviewed, including the protection of hydroxyl and amino groups, the modification of glycosyl groups, the modification of bases, the coupling of glycosyl to bases and the synthesis of oligonucleotides. As a kind of green soft media material with physicochemical property “designable”, ionic liquids are used in the chemical synthesis of nucleosides, which not only increases the solubility of nucleoside compounds but also improves the synthesis efficiency of nucleoside analogues, Toxicity from organic solvents.