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An Urgent Industrial Scheme both for Total Synthesis, and for Pharmaceutical Analytical Analysis of Umifenovir as an Anti-Viral API for Treatment of COVID-19

Author(s):

Akbar Dadras, Mohammad Amin Rezvanfar, Abolghasem Beheshti, Sedigheh Sadat Naeimi and Seyyed Amir Siadati*  

Abstract:


Background: This paper is prepared to reveal about an urgent industrial scheme for a fast and facile total synthesis of umifenovir (arbidol) (by one-pot stages) as an antiviral agent for treating 2019-nCoV virus via inhibiting its viral replication in the human cells. As COVID-19, takes thousands of lives all around the world, it seems that the medicinal resources would not be enough to supply billions of peoples, currently living on the planet earth. Thus, this pandemic and its subsequent impacts on the natural order of our life, would be one of the most important threats against the entire human race.

Aims & Objective: Due to this, in this project, we have made attempts to find an operative approach for synthesizing this compound as an active pharmaceutical ingredient (API), which showed it could be effective in inhibiting the newly emerged coronavirus.

Results: The designed scheme uses relatively cheap precursors, and contains one pot stages, instead of seven time consuming, and more costly, linear steps. Also, it is tried to use safe and cheap solvents like water, and ethanol, instead of toxic ones like methanol, and pyridine which could cause rejection of the API in the organic volatile impurities (OVI) test of pharmacopeia analysis, as well as increasing the concern of inflammability, explosive, and carcinogenic properties of those common solvents.

Conclusion: The most important pharmaceutical analytical methods containing OVI test (mainly ethanol (about 171 ppm) much lower than the limits, by gas chromatography-Flame Ionization Detector (GC-FID) instrument), Assay content (about 99.6% by potentiometric titration), and related purity analysis (by High performance liquid chromatography-Ultraviolet Detector (HPLC-UV)) (about 99.8%) were performed and described to give a more clear industrial scheme.

Keywords:

umifenovir, total synthesis, COVID-19 antiviral, GC-FID, HPLC, Potentiometric titration

Affiliation:

R&D Department, Tofigh Daru Research and Engineering Company, TPICO, Tehran, , Toxicology and Diseases Group (TDG), Pharmaceutical Sciences Research Center (PSRC), The Institute of Pharmaceutical Sciences (TIPS), Tehran University of Medical Sciences, Tehran, , Department of Chemistry, Payame Noor University, Tehran, , R&D Department, Tofigh Daru Research and Engineering Company, TPICO, Tehran, , R&D Department, Tofigh Daru Research and Engineering Company, TPICO, Tehran



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