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Continuous-Flow Synthesis of the Nucleobase Unit of Remdesivir
25 Jun 2024 | Contributor(s):: Guo, Yongxing, Liu, Minjie, Jiang, Meifen, Tao, Yuan, Cheng, Dang, Chen, Fen-Er
In this work, the nucleobase unit of the antiviral drug remdesivir, 7-bromopyrrolo[2,1-f][1,2,4]triazin-4-amine, was synthesized through five-step continuous flow. By adapting batch synthetic chemistry, 7-bromopyrrolo[2,1-f][1,2,4]triazin-4-amine was successfully produced through sequential flow...
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Flash Chemistry Approach to Organometallic C-Glycosylation for the Synthesis of Remdesivir
25 Jun 2024 | Contributor(s):: Keutz, Timo von, Williams, Jason D., Kappe, C. Oliver
In a rapidly changing environment, such as the current COVID-19 pandemic, continuous flow reactors bear the potential to increase the production of urgently needed active pharmaceutical ingredients (APIs) on demand. In the synthesis of remdesivir, the organometallic C-glycosylation step was...
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Development of a Large-Scale Cyanation Process Using Continuous Flow Chemistry En Route to the Synthesis of Remdesivir
25 Jun 2024 | Contributor(s):: Vieira, Tiago, Stevens, Andrew C., Chtchemelinine, Andrei, Gao, Detian, Badalov, Pavel, Heumann, Lars
The implementation of cyanation chemistry at manufacturing scales using batch equipment can be challenging because of the hazardous nature of the reagents employed and the tight control of reaction parameters, including cryogenic temperatures, that help to afford acceptable selectivity and...