Abstract
Since early 2020, scientists have strived to find an effective solution to fight SARSâCoVâ2, in particular by developing reliable vaccines that inhibit the spread of the disease and repurposing drugs for combatting its effects on the human body. The antiviral prodrug Remdesivir is still the most widely used therapeutic during the early stages of the infection. However, the current synthetic routes rely on the use of protecting groups, airâsensitive reagents, and cryogenic conditions, thus impeding a costâefficient supply to patients. We have, therefore, focused on the development of a straightforward, direct addition of (hetero)arenes to unprotected sugars. Here we report a silyliumâcatalyzed and completely stereoselective Câglycosylation that initially yields the openâchain polyols, which can be selectively cyclized to provide either the kinetic αâfuranose or the thermodynamically favored ÎČâanomer. The method significantly expedites the synthesis of Remdesivir precursor GSâ441524 after a subsequent Mnâcatalyzed CâH oxidation and deoxycyanation.
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