Authors
Dinesh J Paymode, Flavio SP Cardoso, Toolika Agrawal, John W Tomlin, Daniel W Cook, Justina M Burns, Rodger W Stringham, Joshua D Sieber, B Frank Gupton, David R Snead
Publication date
2020/9/15
Journal
Organic Letters
Volume
22
Issue
19
Pages
7656-7661
Publisher
American Chemical Society
Description
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.
Scholar articles
DJ Paymode, FSP Cardoso, T Agrawal, JW Tomlin… - Organic Letters, 2020