贵州医科大学学报

2018, v.43;No.217(10) 1198-1202+1208

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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
Synthesis and Process of Metabolites of the New Drug Tyrophentide(Y101)-an Anti-hepatitis B Candidate

杨方红;曾晓萍;徐峰;梁光义;徐必学;
YANG Fanghong;ZENG Xiaoping;XU Feng;LIANG Guangyi;XU Bixue;College of Pharmacy,Guizhou University;State Key Laboratory of Functions and Applications of Medicinal Plants,Guizhou Medcial University;The Key Laboratory of Chemistry for Natural Products of Guizhou Province and Chinese Academy of Sciences;

摘要(Abstract):

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 drug 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 structures of the synthesized compounds were confirmed by1 H NMR,13 C NMR and ESI-MS,and the purity of M8 and M9 were analyzed through high performance 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.

关键词(KeyWords): 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

Abstract:

Keywords:

基金项目(Foundation): 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]

作者(Author): 杨方红;曾晓萍;徐峰;梁光义;徐必学;
YANG Fanghong;ZENG Xiaoping;XU Feng;LIANG Guangyi;XU Bixue;College of Pharmacy,Guizhou University;State Key Laboratory of Functions and Applications of Medicinal Plants,Guizhou Medcial University;The Key Laboratory of Chemistry for Natural Products of Guizhou Province and Chinese Academy of Sciences;

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DOI: 10.19367/j.cnki.1000-2707.2018.10.015

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