恩曲他滨对映异构体的合成、表征及HPLC分析  

Synthesis,characterization and HPLC analysis of enantiomer of emtricitabine

作　　者：汤君[1] 何彩玉[2] 程杰[1] 柏俊[1] 

机构地区：[1]安徽省药物研究所,安徽合肥230022 [2]安徽中医药大学,安徽合肥230031

出　　处：《化学研究与应用》2014年第2期294-297,共4页Chemical Research and Application

摘　　要：以(1′R,2′S,5′R)-薄荷基-5R-乙酰基-1,3-氧硫杂环戊烷-2S-羧酸酯为原料,经偶联、还原两步反应制得恩曲他滨对映异构体,总收率约59%。其结构及绝对构型经~1H NMR、^(13)C NMR、HPLC、ESI-MS和比旋光度确证。建立恩曲他滨与其对映异构体的HPLC分析方法,可用于恩曲他滨原料药的手性质量控制。The emtricitabine enantiomer in an overall yield of 59%was synthesized from（1′R,2S,5′R）-menthyl-5R-acetoxy-1,3-ox-athiolane-2S-carboxylate over coupling reaction and reduction reaction.The structure and absolute configuration of emtricitabine en-antiomer was confirmed by 1 H NMR、13 C NMR、HPLC、ESI-MS and specific rotation.The HPLC analysis method of emtricitabine and its enantiomer was established to apply to chiral control for Emtricitabine API.

关 键 词：恩曲他滨 对映异构体 高效液相色谱 手性控制 绝对构型 

分 类 号：O621.3[理学—有机化学]