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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Bibliographic Details
Main Authors: Seyyed Amir Siadati, Mehdi Soheilizad, Loghman Firoozpour, Marjan Samadi, Meghdad Payab, Saeed Bagherpour, Seyyed Mehdi Mousavi
Format: Article
Language:English
Published: Hindawi Limited 2022-01-01
Series:Journal of Chemistry
Online Access:http://dx.doi.org/10.1155/2022/8759235
Description
Summary: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.
ISSN:2090-9071