A High-Yielding Synthesis of EIDD-2801 from Uridine.
Alexander SteinerDesiree ZnidarSándor B ÖtvösDavid R SneadDoris DallingerC Oliver KappePublished in: European journal of organic chemistry (2020)
A simple reordering of the reaction sequence allowed the improved synthesis of EIDD-2801, an antiviral drug with promising activity against the SARS-CoV-2 virus, starting from uridine. Compared to the original route, the yield was enhanced from 17 % to 61 %, and fewer isolation/purification steps were needed. In addition, a continuous flow procedure for the final acetonide deprotection was developed, which proved to be favorable toward selectivity and reproducibility.