瑞德西韦的合成方法

Synthesis of Remdesivir

目的 建立适合大规模产业化制备瑞德西韦的合成方法。方法 对化合物4的制备工艺进行优化,以叔丁基二苯基氯硅烷(TBDPSiCl)进行保护,增加产品反应转化率,提高产品光学纯度。结果 所制得的化合物经液相色谱-质谱联用(LC-MS)、氢谱核磁共振(1H-NMR)和碳谱核磁共振(13C-NMR)进行结构确证,与目标化合物的结构相符。该合成方法包含六步反应,总收率为21.3%。结论 该方法可作为瑞德西韦大规模产业化的合成方法。

Objective To establish a synthetic method suitable for the large-scale industrial preparation of remdesivir.Methods T-butyldiphenylchlorosilane(TBDPSiCl)as specific in-situ protection was used to optimize the synthesis procedure of compound 4 to enhance the conversion rate and the optical purity of the product.Results The structure of the compound obtained by this method was confirmed by LC-MS,1 H-NMR and13 C-NMR,and the result was consistent with that of the target compound.The synthesis method consisted of six steps with a total yield of 21.3%.Conclusion This method can be used as the large-scale industrialization synthesis method of remdesivir.