A review of the synthetic strategies toward the antiviral drug tecovirimat

• Published in: Organic & biomolecular chemistry 2024-09
• Main Authors: Bonku, Emmanuel Mintah, Qin, Hongjian, Odilov, Abdullajon, Abduahadi, Safomuddin, Guma, Samuel Desta, Zhu, Fuqiang, Shen, Jingshan
• Format: Article
• Language: English
• ISSN: 1477-0520; 1477-0539; 1477-0539
• DOI: 10.1039/d4ob01092b

This review provides a comprehensive analysis of synthetic routes for tecovirimat, an antiviral drug used to treat orthopoxvirus infections, including monkeypox and smallpox. We focus on the scale-up synthesis of key intermediates, including cycloheptatriene, as documented in the published literature and patent records. The review highlights the efficiency, yield, and purity of these approaches, as well as the minimization of genotoxic and in-process impurities. Furthermore, we critically evaluate the recently reported optimized industrial-scale synthesis process, highlighting its advantages and limitations, and identifying avenues for further improvement. By obtaining insights from the published literature and patent records, this review elucidates the current state of knowledge regarding key synthesis parameters influencing tecovirimat production and emphasizes the critical importance of optimizing synthesis techniques to achieve remarkable improvements in safety and environmental impact. This review serves as a valuable resource for researchers and industry professionals in the field of R&D and production of APIs, particularly in expediting the safe and efficient industrial production of tecovirimat.