A facile multicomponent, catalyst-free oxazolidinone synthesis from primary aliphatic or aromatic amines and dibromoethane is described. It relies on the usage of cesium carbonate or cesium hydrogencarbonate as the simultaneous base and C1 source...
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Synthesis of Remdesivir by Direct Lithiation of Pyrrolo[2,1‐f][1,2,4]triazine Derivatives Enabled C‐Glycosylation
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A direct and regioselective lithiation was realized on N-Boc-pyrrolo[2,1-f][1,2,4]triazine, simply utilizing the distinct sigma-acidity on C-9. Starting from this enabling discovery, C-glycoside formation, cyanation, and global deprotection steps constitute one of the most efficient syntheses of GS-441524. Furthermore, transient protection was applied on GS-441524 with phenyl boronic acid, which facilitated a powerful one-pot synthesis of remdesivir.
Abstract
A direct and regioselective lithiation was realized on N-Boc-pyrrolo[2,1-f][1,2,4]triazine, simply utilizing the distinct sigma-acidity on C-9. Starting from this enabling discovery, C-glycoside formation, cyanation, and global deprotection steps constitute one of the most efficient syntheses of GS-441524. Furthermore, transient protection was applied on GS-441524 with phenyl boronic acid, which facilitated a powerful one-pot synthesis of remdesivir.
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