Synthesis of Remdesivir Derivate as a Generation of Anti-COVID-۱۹ Drugs Through Acetylation Reactions

Remdesivir, a competitive inhibitor of viral RNA-dependent RNA polymerase, is the drug of choice for anti-COVID-۱۹ treatment. However, the instability of these substances in plasma raises doubts about their therapeutic potency. Additionally, SARS-CoV-۲-infected cells may exhibit a variety of antiviral behaviors due to intricate activation pathways. Therefore, this study aimed to develop a synthesis for the remdesivir derivative.The remdesivir derivative was synthesized using acetyl chloride as a reagent in a ratio of ۱:۳ in dichloromethane and tetrahydrofuran solvent at ۳۰°C for ۶ h. Thin-layer chromatography and spectrophotometers (۱H NMR and ۱۳C NMR) were used to identify the produced molecule, which was a brownish-yellow crystalline powder. The results of the synthesis yielded ۰.۸ gr (۷۷.۳۴%), and the Rf value of the remdesivir derivate was ۰.۵۴. The characterization with ۱H NMR at δ۲.۵ ppm (۳H, s) indicated the presence of a proton in the H-C-C=O structure caused by the substitution of the acetyl group in the remdesivir structure. The ۱۳C NMR data indicated the presence of aromatic carbons, alkenes, C≡N, and carbon bonds with electronegative O. This remdesivir derivate chemical can be a potential candidate for an anti-COVID-۱۹ drug that has more potency because it has substitutions of acetyl groups at positions ۲' and ۳' in the structure of remdesivir.

Keywords:

Acetylation , Acetyl chloride , covid-۱۹ , Remdesivir , Remdesivir Derivate , Synthesis