瑞德西韦中间体合成工艺研究

Synthesis of Intermediate of Remdesivir

以2-乙基-1-丁醇和L-丙氨酸为起始原料,经酯化反应、胺化反应和羟基化反应合成瑞德西韦中间体,同时考察了催化剂类型、催化剂用量、缚酸剂类型、反应溶剂和反应温度等因素对产品的收率和纯度的影响,确定了最佳工艺条件,总收率40%,纯度99.6%,其结构经1H-NMR和MS表征。该方法具有原料易得、反应条件温和、操作简便、成本低廉、环境友好等优点,适合工业化生产。

The intermediate of remdesivir was synthesized from 2-ethyl butanol and L-alanine by esterification,amination and hydroxylation reaction,the reaction conditions,such as catalyst type,catalyst amount,acid binding agent type,reaction solvent and reaction temperature,were examined to give the preferable process,the total yield was 40%,purity was 99.6%.The structure was characterized by 1H-NMR and MS.This method has the advantages of easy to obtain raw materials,mild reaction conditions,simple operation,low cost and environmental friendliness,and is suitable for industrial production.