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Expanding Access to Remdesivir via an Improved Pyrrolotriazine Synthesis: Supply Centered Synthesis

[Image: see text] Pyrrolotriazine 1 is an important precursor to remdesivir. Initial results toward an efficient synthesis are disclosed consisting of sequential cyanation, amination, and triazine formation beginning from pyrrole. This route makes use of highly abundant, commoditized raw material in...

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Detalles Bibliográficos
Autores principales: Paymode, Dinesh J., Cardoso, Flavio S. P., Agrawal, Toolika, Tomlin, John W., Cook, Daniel W., Burns, Justina M., Stringham, Rodger W., Sieber, Joshua D., Gupton, B. Frank, Snead, David R.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2020
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7536717/
https://www.ncbi.nlm.nih.gov/pubmed/32931286
http://dx.doi.org/10.1021/acs.orglett.0c02848
Descripción
Sumario:[Image: see text] Pyrrolotriazine 1 is an important precursor to remdesivir. Initial results toward an efficient synthesis are disclosed consisting of sequential cyanation, amination, and triazine formation beginning from pyrrole. This route makes use of highly abundant, commoditized raw material inputs. The yield of triazine was doubled from 31% to 59%, and the synthetic step count was reduced from 4 to 2. These efforts help to secure the remdesivir supply chain.