Resources (1-3 of 3)

1. Flash Chemistry Approach to Organometallic C-Glycosylation for the Synthesis of Remdesivir

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   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...

2. Using Flow To Outpace Fast Proton Transfer in an Organometallic Reaction for the Manufacture of Verubecestat (MK-8931)

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   25 Jun 2024 | Contributor(s):: Thaisrivongs, David A., Naber, John R., McMullen, Jonathan P.

   We report that an organolithium addition to a chiral ketimine, which because of competitive proton transfer proceeds with only modest yield in batch, can be significantly improved in flow. The transformation was discovered to be highly mixing-sensitive but remarkably temperature-independent in...

3. Continuous Flow C-Glycosylation via Metal-Halogen Exchange: Process Understanding and Improvements toward Efficient Manufacturing of Remdesivir

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   09 Jun 2023 | Contributor(s):: von;Keutz, T, Williams, JD, Kappe, CO

   As remdesivir is the first approved treatment for COVID-19 (SARS-CoV-2), its production is likely to be of vital importance in the near future. Continuous flow processing has been demonstrated as a key technology in the manufacturing of highvolume active pharmaceutical ingredients and is...