Chemical Synthesis of the Anti‐COVID‐19 Drug Remdesivir

Abstract

Remdesivir has become an important compound for the treatment of COVID-19. Here, we describe the catalytic asymmetric synthesis of this anti-COVID-19 drug. First, the P-racemic phosphoryl chloride is synthesized in a facile procedure. Then, it is possible to obtain the protected remdesivir via the organocatalytic asymmetric phosphorylation of protected nucleoside GS441524 with Pracemic phosphoryl chloride catalyzed by chiral bicyclic imidazole. Finally, remdesivir is easily prepared by deprotection.

Synthesis of 1,2-oxaphosphinane 2-oxides and 1,2-oxaphosphinine 2-oxides: δ-phosphonolactones and δ-phosphinolactones

“…Thus, new synthetic strategies are in demand for highly enantioselective synthesis of enantiopure 1,2-oxaphosphinane and 1,2-azaphosphinine 2-oxides and will be developed along with success in asymmetric catalysis for the synthesis of optically active phosphorus compounds. 115…”