Pyrrolo[2,1-f][1,2,4]triazine (1) is an important regulatory starting material in the production of the antiviral drug remdesivir. Compound 1 was produced through a newly developed synthetic methodology utilizing simple building blocks such as pyrrole, chloramine, and formamidine acetate by examining the mechanistic pathway for the process optimization exercise. Triazine 1 was obtained in 55% overall yield in a two-vessel-operated process. This work describes the safety of the process, impurity profiles and control, and efforts toward the scale-up of triazine for the preparation of kilogram quantity.

中文翻译：

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Remdesivir 的 Pyrrolo[2,1-f][1,2,4]三嗪的简便且可扩展的方法

Pyrrolo[2,1- f ][1,2,4]triazine ( 1 ) 是生产抗病毒药物 remdesivir 的重要监管起始材料。化合物1是通过一种新开发的合成方法生产的，该方法利用简单的结构单元，如吡咯、氯胺和醋酸甲脒，通过检查工艺优化活动的机制途径。在双容器操作的过程中，三嗪1的总产率为 55%。这项工作描述了该工艺的安全性、杂质分布和控制，以及为按比例放大三嗪以制备千克量的努力。