一种瑞德西韦非对映异构体的合成及其高效液相分析

Synthesis of a Diastereomer of Remdesivir and its HPLC Analysis

目的:本论文通过对瑞德西韦非对映异构体REMD-A进行合成研究,为瑞德西韦的质控标准提供参考。方法:首先以4-氨基吡咯并[2,1-f][1,2,4]-三嗪为起始原料,经过7步反应得到非对映异构体REMD-A。结果:该工艺可以快速制备高纯度中间体REMD-005-A,通过该中间体可以制备得到高纯度的REMD-A。结论:瑞德西韦制备过程中可能存在非对映异构体。本文提供了其制备方法和高效液相分析方法,为瑞德西韦异构体杂质控制提供了依据。

Objective:This thesis provides a reference for its quality control standards through the synthesis of REMD-A(a diastereomer of Remdesivir).Methods:Firstly,4-aminopyrrolo[2,1-f][1,2,4]-triazine was used as the starting material,and the REMD-A was obtained after 7 steps of reaction.Results:The process can quickly prepare the high-purity intermediate REMD-005-A,through which the high-purity REMD-A can be prepared.Conclusion:There may be diastereomers in the preparation process of Remdesivir.This article presents its preparation method and HPLC analysis method to provide a basis for the control of Remdesivir isomers.