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submitted on 01.08.2020 and posted on 10.08.2020by Dinesh
J. Paymode, Flavio
S. P. Cardoso, Joshua D. Sieber, John W. Tomlin, Daniel W. Cook, Justina Burns, Rodger W. Stringham, B. Frank Gupton, David Snead, Toolika Agrawal
is an important precursor to Remdesivir, and an efficient synthesis is disclosed. This
route features atom economy and reduced derivatization of starting materials,
by making 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. A one-pot cascade sequence was developed for
direct cyanation of pyrrole. Amination
and cyclization with formamidine acetate complete the synthesis. The
problematic nature of typically dilute electrophilic aminations was solved with
semi-continuous processing. Moreover,
development of a continuous platform afforded access to the ideal yet
non-commercial aminating reagent, monochloramine. These efforts help to secure the Remdesivir