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.
出处
《化学研究与应用》
CAS
CSCD
北大核心
2014年第2期294-297,共4页
Chemical Research and Application
