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目的探索更有效的合成salac inol及其衍生物的方法,以研发新的糖尿病治疗药。方法以D-葡萄糖为原料,经7步反应制得salac inol及其衍生物合成的关键中间体2,4-O-异丙亚基-L-赤藓糖醇-1,3-环硫酸酯(2a);此方法成本明显低于文献报道的以L-葡萄糖为原料的合成方法。以此方法,制备salac inol的含氮衍生物4,并与salac inol进行了体外抑制α-葡糖苷酶活性的比较研究。结果采用此种新的路线,顺利制得salac inol的含氮衍生物(4)及结构简化物(13)。结论以D-葡萄糖为原料的新的合成路线优于文献方法,salac inol分子结构中的硫原子用氮原子替代时,其活性明显降低。
Objective To explore a more effective method for the synthesis of salac inol and its derivatives to develop new therapeutic drugs for diabetes. Methods Using D-glucose as raw material, the key intermediate of salac inol and its derivatives, 2,4-O-isopropylidene-L-erythritol-1,3-cyclic sulfate (2a). The cost of this method is obviously lower than that reported in the literature using L-glucose as a raw material. In this way, the nitrogen-containing derivative 4 of salac inol was prepared and compared with salac inol for the comparative inhibition of the α-glucosidase activity. Results Using this new route, the nitrogen-containing derivative of salac inol (4) and the structural simplification (13) were successfully obtained. Conclusion The new synthetic route using D-glucose as raw material is superior to the literature method. The sulfur atom in salac inol molecular structure is obviously reduced when it is replaced by nitrogen atom.