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“一锅法”制备索菲布韦中间体

One-pot Synthesis of Intermediate of Sofosbuvir

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【作者】 叶连宝吴杰杨杰波陈伟强

【Author】 YE Lian-bao;WU Jie;YANG Jie-bo;CHEN Wei-qiang;College of Pharmacy,Guangdong Pharmaceutical University;

【机构】 广东药学院药科学院

【摘要】 以L-丙氨酸异丙酯盐酸盐、苯基二氯磷酸酯、2,3,4,5,6-五氟苯酚为原料,通过"一锅法"经磷酰化反应得到治疗丙肝药物中间体——索菲布韦中间体(2-[(S)-(2,3,4,5,6-五氟苯氧基)-苯氧磷酰胺基]丙酸异丙酯)。目标化合物经1HNMR、MS确认结构,总产率53%。该方法为标题化合物的合成提供了一条较为合理的路线。

【Abstract】 To synthesize intermediate of sofosbuvir 2-[( S)-( 2,3,4,5,6-pentafluoro-phenoxy) phenoxyphosphorylamino]propionic acid isopropyl ester by one-pot reaction. The 2-[( S)-( 2,3,4,5,6-pentafluoro-phenoxy) phenoxyphosphorylamino]propionic acid isopropyl ester was synthesized using L-alanine isopropyl ester hydrochloride,phenyl dichlorophosphate,2,3,4,5,6-pentafluoro phenol as materials via phosphorylation reaction by one-pot method. The chemical structure of the target compound was confirmed by MS and1 HNMR. The overall yield of title compound was 53%. This work can provide a more reasonable route for the production of 2-[( S)-( 2,3,4,5,6-pentafluoro-phenoxy) phenoxyphosphorylamino]propionic acid isopropyl ester.

  • 【分类号】R914.5
  • 【被引频次】3
  • 【下载频次】616
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