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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. © 2021 Sociedade Brasileira de Quimica.

Klein’s Remdesivir-Nucleobase Synthesis Revisited: Chemoselective Cyanation of Pyrrol-2-carboxaldehyde