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氟苯尼考的合成工艺研究
Improved synthesis of florfenicol
【摘要】 目的研究氟苯尼考的合成工艺。方法以(1R,2R)-3-羟基-2-氨基-3-[4-(甲砜基)苯基]-丙酸乙酯为原料,经过还原、保护、氟化、水解、二氯乙酰化5步反应最后得到氟苯尼考。结果与结论该合成路线简单,原料易得,目标化合物的总收率为78%。
【Abstract】 Aim To improve a synthetic route of florfenicol.Methods The target compound was synthesized by using(1R,2R)-3-hydroxy-2-amino3-[4-(methylsulfonyl)-phenyl]-ethyl propionate as starting material,via a five steps process including reduction,protection,fluorination,hydrolyzation,dichloroacetylation.Results and conclusion The starting materials in the synthetic route are easily available and the total yield is 78%.The synthetic procedure of intermediates 3-6 were improved.
- 【文献出处】 中国药物化学杂志 ,Chinese Journal of Medicinal Chemistry , 编辑部邮箱 ,2007年03期
- 【分类号】TQ463.2
- 【被引频次】5
- 【下载频次】1383