An Industrial Approach to Production of Tofacitinib Citrate (TFC) as an Anti-COVID-19 Agent: A Joint Experimental and Theoretical Study

In this report, we have presented our experience about a facile method for synthesis of tofacitinib citrate (TFC). The developed analytical methods for identification and qualifications are also included. As TFC seems to be effective in treatment of the symptoms of COVID-19 (SARS family), manufactur...

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Main Authors: Seyyed Amir Siadati, Mehdi Soheilizad, Loghman Firoozpour, Marjan Samadi, Meghdad Payab, Saeed Bagherpour, Seyyed Mehdi Mousavi
Format: Article
Language:English
Published: Wiley 2022-01-01
Series:Journal of Chemistry
Online Access:http://dx.doi.org/10.1155/2022/8759235
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author Seyyed Amir Siadati
Mehdi Soheilizad
Loghman Firoozpour
Marjan Samadi
Meghdad Payab
Saeed Bagherpour
Seyyed Mehdi Mousavi
author_facet Seyyed Amir Siadati
Mehdi Soheilizad
Loghman Firoozpour
Marjan Samadi
Meghdad Payab
Saeed Bagherpour
Seyyed Mehdi Mousavi
author_sort Seyyed Amir Siadati
collection DOAJ
description In this report, we have presented our experience about a facile method for synthesis of tofacitinib citrate (TFC). The developed analytical methods for identification and qualifications are also included. As TFC seems to be effective in treatment of the symptoms of COVID-19 (SARS family), manufacturing of this active pharmaceutical ingredient (API) could be helpful. The API of TFC was prepared from the diamine intermediate in an ambient and solvent-free condition. Elimination of the reaction solvent resulted in decreasing the cost and preventing the rejection of the organic volatile impurity (OVI) test. The final citrate addition step was carried out using water as a solvent (the citrate content was 37.5% by potentiometry). Moreover, the results of the Karl-Fischer (KF) titration analysis was about 0.24%, which showed that the use of water does not increase the water content of the crystal structure.
format Article
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institution Kabale University
issn 2090-9071
language English
publishDate 2022-01-01
publisher Wiley
record_format Article
series Journal of Chemistry
spelling doaj-art-e1df87414d9b433886239b23eaffdf022025-02-03T00:59:37ZengWileyJournal of Chemistry2090-90712022-01-01202210.1155/2022/8759235An Industrial Approach to Production of Tofacitinib Citrate (TFC) as an Anti-COVID-19 Agent: A Joint Experimental and Theoretical StudySeyyed Amir Siadati0Mehdi Soheilizad1Loghman Firoozpour2Marjan Samadi3Meghdad Payab4Saeed Bagherpour5Seyyed Mehdi Mousavi6Department of Research & DevelopmentDepartment of Research & DevelopmentDepartment of Research & DevelopmentDepartment of Research & DevelopmentFaculty of ChemistryDepartment of Research & DevelopmentDepartment of Research & DevelopmentIn this report, we have presented our experience about a facile method for synthesis of tofacitinib citrate (TFC). The developed analytical methods for identification and qualifications are also included. As TFC seems to be effective in treatment of the symptoms of COVID-19 (SARS family), manufacturing of this active pharmaceutical ingredient (API) could be helpful. The API of TFC was prepared from the diamine intermediate in an ambient and solvent-free condition. Elimination of the reaction solvent resulted in decreasing the cost and preventing the rejection of the organic volatile impurity (OVI) test. The final citrate addition step was carried out using water as a solvent (the citrate content was 37.5% by potentiometry). Moreover, the results of the Karl-Fischer (KF) titration analysis was about 0.24%, which showed that the use of water does not increase the water content of the crystal structure.http://dx.doi.org/10.1155/2022/8759235
spellingShingle Seyyed Amir Siadati
Mehdi Soheilizad
Loghman Firoozpour
Marjan Samadi
Meghdad Payab
Saeed Bagherpour
Seyyed Mehdi Mousavi
An Industrial Approach to Production of Tofacitinib Citrate (TFC) as an Anti-COVID-19 Agent: A Joint Experimental and Theoretical Study
Journal of Chemistry
title An Industrial Approach to Production of Tofacitinib Citrate (TFC) as an Anti-COVID-19 Agent: A Joint Experimental and Theoretical Study
title_full An Industrial Approach to Production of Tofacitinib Citrate (TFC) as an Anti-COVID-19 Agent: A Joint Experimental and Theoretical Study
title_fullStr An Industrial Approach to Production of Tofacitinib Citrate (TFC) as an Anti-COVID-19 Agent: A Joint Experimental and Theoretical Study
title_full_unstemmed An Industrial Approach to Production of Tofacitinib Citrate (TFC) as an Anti-COVID-19 Agent: A Joint Experimental and Theoretical Study
title_short An Industrial Approach to Production of Tofacitinib Citrate (TFC) as an Anti-COVID-19 Agent: A Joint Experimental and Theoretical Study
title_sort industrial approach to production of tofacitinib citrate tfc as an anti covid 19 agent a joint experimental and theoretical study
url http://dx.doi.org/10.1155/2022/8759235
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