稳定同位素标记的Y101及其代谢产物的合成  

Synthesis of Stable Isotope Labeled Y101 and its Metabolites

作　　者：童洋[1,2,3] 曾晓萍[2,3] 陈小敏[2,3] 梁光义[1,2,3] 徐必学[2,3] 

机构地区：[1]贵阳中医学院药学院,贵州贵阳550002 [2]贵州医科大学省部共建药用植物功效与利用国家重点实验室,贵州贵阳550014 [3]贵州省中国科学院天然产物化学重点实验室,贵州贵阳550014

出　　处：《化学试剂》2017年第8期879-883,共5页Chemical Reagents

基　　金：国家自然科学基金资助项目(81360472);西部之光人才培养计划(2014)

摘　　要：以氘代甲苯为原料,经高锰酸钾氧化反应生成氘代苯甲酸,再经缩合、烷基化、水解等反应,合成了N-(N-苯甲酰基-O-二甲氨基乙基-L-酪氨酰基)-L-苯丙氨醇及其代谢产物M-8、M-9的稳定同位素标记化合物。所得化合物均经核磁(NMR)、质谱(ESI-MS)进行结构确证。样品可作为生物内标,用于高效液相色谱/质谱联用法对目标化合物及其代谢产物在体内的定量分析,同时开展了该化合物的体内代谢研究。Using deuterium-substituted toluene as starting material, deuterium labeled N- [ N-benzoyl-O- （ 2-dimethyl-aminoethyl ） - L-tyrosyl]-L-phenylalaninol was synthesized by oxidation with potassium permanganate, sequentially condensation with L-tyrosine and L-phenylalaninol, alkylation with 2-dimethylaminoethyl chloride hydrochloride.Deuterium labeled metabolic products M-8 and M-9 were also prepared in similar methods.The structures of all the synthesized compounds were confirmed by ESI-MS and NMR spectroscopy.The deuterium labeled target compound, M-8 and M-9 can be used as internal standard for quantitative analysis using high performance liquid chromatography/mss spectrometry （HPLC/MS） in the metabolic study of that compound.

关 键 词：Y101 同位素标记 代谢途径 

分 类 号：TQ421.6[化学工程]