目的：对马蹄金素衍生物（研发代号Y101）代谢产物M8、M9的合成工艺进行优化并制备合格样品。方法：以L-酪氨酸甲酯盐酸盐为原料,设计不同的合成工艺,经过酰化、水解、苄基化、烷基化、催化氢化、N-氧化等反应合成替芬泰的主要代谢产物M8、M9,所得化合物经^1H NMR,^13C NMR,ESI-MS进行结构确证,并用高效液相色谱对其进行分析检测。结果：完成了M8、M9合成工艺路线的选择与优化,制备了合格的M8和M9样品。结论：优选的合成工艺制备所得的M8、M9样品纯度达到了95%以上。
Objective： To design and optimize a synthetic route for the synthesis of M8 and M9 and the metabolites of the new drag Tyrophentide （Y101）-an anti-hepatitis B candidate , so as to prepare qualified M8 and M9 for further study. Methods ： Two different synthetic routes were designed for the synthesis of M8 and M9 using L-tyrosine methyl ester hydrochloride as the starting material by acylation, hydrolysis, benzylation, alkylation, catalytic hydrogenation and N-oxidation reaction. The structurs of the synthesized compounds were confirmed by ^1H NMR, ^13C NMR and ESI-MS, and the purity of M8 and M9 were analyzed through high pefformance liquid chromatography （HPLC）. Results： A synthetic route for the large scale synthesis of M8 and M9 was developed and used for the preparation of qualified samples of M8 and M9. Conclusion： The purity of M8 and M9 prepared for the optimized synthetic route was more than 95%. The obtained samples can be used for the biological activities and toxicity detection of M8 and M9.
Journal of Guizhou Medical University
L- tyrosine methyl ester hydrochloride