氘代肌酸的新合成方法  

A new synthesis method of deuterated creatine

作　　者：李西恒 周欣梅 胡泽涛 何新华 任旭红[1] LI Xiheng;ZHOU Xinmei;HU Zetao;HE Xinhua;REN Xuhong(Shenyang Pharmaceutical University Faculty of Pharmaceutical Engineering,Shenyang 110016,China;Academy of Military Medical Sciences,Institute of Poison and Drug Research,Beijing 100850,China)

机构地区：[1]沈阳药科大学制药工程学院,辽宁沈阳110016 [2]军事科学院军事医学研究院毒物药物研究所,北京100850

出　　处：《沈阳药科大学学报》2023年第10期1291-1294,1305,共5页Journal of Shenyang Pharmaceutical University

基　　金：辽宁省教育厅基础研究项目(2020LJC08)。

摘　　要：目的氘代肌酸可作为临床样品检测和分析的内标基准物质,研究以高收率获得氘代肌酸的合成方法。方法以N-苄基甘氨酸乙酯和氘代碘甲烷为原料,经过亲核取代、催化氢化、脱苄基保护、Boc-胍基取代、水解反应和脱Boc保护五步反应得到产物。结果以33.0%收率得到氘代肌酸。结论所得产物经HPLC检测,纯度为99.9%,总收率为33.0%,结构经MS、^(1)H-NMR和^(13)C-NMR确认。purpose:Creatine,also known asα-methylguanidine acetic acid,is a naturally occurring nutrient in human body and has a variety of biological functions.Deuterium creatine can be used as internal reference material for clinical sample detection and analysis.objective:Deuterated creatine was obtained with high yield.method:In this paper,n-benzyl glycine ethyl ester and deuterium iodide methane were used as raw materials to obtain the product in high yield through five steps of nucleophilic substitution,catalytic hydrogenation,debenzyl protection,BOC-guanidine replacement,hydrolysis and deboc protection.Result:Deuterated creatine was obtained with a high yield of 33.0%.conclusion:The purity of the product was 99.9%by HPLC and the total yield was 33.0%.The structure of the product was confirmed by MS,^(1)H-NMR and^(13)C-NMR.

关 键 词：肌酸 氘代肌酸 合成 苄基保护 

分 类 号：R914[医药卫生—药物化学]