Klein’s Remdesivir-Nucleobase Synthesis Revisited: Chemoselective Cyanation of Pyrrol-2-carboxaldehyde
AUTOR(ES)
Santos, Juliana A. dos; Pereira, Vinícius R. D.; Silva, Adilson D. da; Amarante, Giovanni W.
FONTE
J. Braz. Chem. Soc.
DATA DE PUBLICAÇÃO
2021-07
RESUMO
4-Aminopyrrolo[2,1-f][1,2,4]triazine is a fundamental raw material in the synthesis of remdesivir, which demand has increased due to the tests and potential repositioning of this drug against Coronavirus disease 2019 (COVID-19). Here, three chemical steps route for the preparation of remdesivir’s nucleobase is described. Particularly, a highly chemoselective cyanation of Klein’s route and successful application of monochloramine prepared from commercial bleach as an N-amination reagent are presented.
