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抗乙肝候选新药替芬泰代谢产物M8和M9的合成工艺研究 预览 被引量:2

Synthesis and Process of Metabolites of the New Drug Tyrophentide ( Y101 ) -an Anti-hepatitis B Candidate
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摘要 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.
作者 杨方红 曾晓萍 徐峰 梁光义 徐必学 YANG Fanghong1,2,3, ZENG Xiaoping2,3 , XU Feng2,3 , LIANG Guangyi2,3 , XU Bixue2,3(1. College of Pharmacy, Guizhou University, Guiyang 550002, Guizhou, China ; 2. State Key Laboratory of Funetions and Applications of Medicinal Plants, Guizhou Medcial University, Guiyang 550014, Guizhou, China; 3. The Key Laboratory of Chemistry for Natural Products of Guizhou Province and Chinese Academy of Sciences, Guiyang 550014, Guizhou, China)
出处 《贵州医科大学学报》 CAS 2018年第10期1198-1202,1208共6页 Journal of Guizhou Medical University
基金 国家自然科学基金资助项目(81760623) 贵州省高层次创新人才项目[黔科合平台人才(2016)5678]
关键词 马蹄金素衍生物 L-酪氨酸甲酯盐酸盐 代谢产物 合成工艺 替芬泰 Matijin-Su derivative L- tyrosine methyl ester hydrochloride metabolites synthesis technology tyrophentide
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