Facile and Scalable Methodology for the Pyrrolo[2,1‑f][1,2,4]triazine of Remdesivir
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 exami...
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| Veröffentlicht in: | Organic process research & development 2022-01, Vol.26 (1), p.82-90 |
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| container_title | Organic process research & development |
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| creator | Roy, Sarabindu Yadaw, Ajay Roy, Subho Sirasani, Gopal Gangu, Aravind Brown, Jack D Armstrong, Joseph D Stringham, Rodger W Gupton, B. Frank Senanayake, Chris H Snead, David R |
| description | 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. |
| doi_str_mv | 10.1021/acs.oprd.1c00071 |
| format | Article |
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| source | ACS Publications |
| title | Facile and Scalable Methodology for the Pyrrolo[2,1‑f][1,2,4]triazine of Remdesivir |
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