4.6 Article

Facile and Scalable Methodology for the Pyrrolo[2,1-f][1,2,4]triazine of Remdesivir

期刊

ORGANIC PROCESS RESEARCH & DEVELOPMENT
卷 26, 期 1, 页码 82-90

出版社

AMER CHEMICAL SOC
DOI: 10.1021/acs.oprd.1c00071

关键词

antiviral agents; API; remdesivir; triazine; supply centered synthesis

资金

  1. Bill and Melinda Gates Foundation

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This study presents a newly developed synthetic methodology for the production of Pyrrolo[2,1-f][1,2,4]triazine, an important starting material for the antiviral drug remdesivir. Through examining the mechanistic pathway, simple building blocks such as pyrrole, chloramine, and formamidine acetate were successfully utilized to obtain triazine 1 with an overall yield of 55% in a two-vessel-operated process. The research also focuses on the safety of the process, impurity profiles and control, and efforts towards scale-up for large-scale production.
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.

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