Increasing global access to the high-volume HIV drug nevirapine through process intensificationElectronic supplementary information (ESI) available. See DOI: 10.1039/c7gc00937b

• Main Authors: Verghese, Jenson, Kong, Caleb J, Rivalti, Daniel, Yu, Eric C, Krack, Rudy, Alcázar, Jesus, Manley, Julie B, McQuade, D. Tyler, Ahmad, Saeed, Belecki, Katherine, Gupton, B. Frank
• Format: Article
• Language: English
• ISSN: 1463-9262; 1463-9270
• DOI: 10.1039/c7gc00937b

Access to affordable medications continues to be one of the most pressing issues for the treatment of disease in developing countries. For many drugs, synthesis of the active pharmaceutical ingredient (API) represents the most financially important and technically demanding element of pharmaceutical operations. Furthermore, the environmental impact of API processing has been well documented and is an area of continuing interest in green chemical operations. To improve drug access and affordability, we have developed a series of core principles that can be applied to a specific API, yielding dramatic improvements in chemical efficiency. We applied these principles to nevirapine, the first non-nucleoside reverse transcriptase inhibitor used in the treatment of HIV. The resulting ultra-efficient (91% isolated yield) and highly-consolidated (4 unit operations) route has been successfully developed and implemented through partnerships with philanthropic entities, increasing access to this essential medication. We anticipate an even broader global health impact when applying this model to other active ingredients. Fundamental elements of process intensification were applied to generate efficient batch and continuous syntheses of the high-volume HIV drug nevirapine.