Optimization and Scale-Up of the Continuous Flow Acetylation and Nitration of 4-Fluoro-2-methoxyaniline to Prepare a Key Building Block of Osimertinib
25 Jun 2024 | Contributor(s):: Köckinger, Manuel, Wyler, Benjamin, Aellig, Christof, Roberge, Dominique M., Hone, Christopher A., Kappe, C. Oliver
The development of a scalable telescoped continuous flow procedure for the acetylation and nitration of 4-fluoro-2-methoxyaniline is described. A subsequent batch deprotection then affords 4-fluoro-2-methoxy-5-nitroaniline, a key building block in the synthesis of osimertinib, a third-generation...
Continuous Multiphase Flow Nitration and Cryogenic Flow Formylation: Enabling Process Development and Manufacturing of Pharmaceutical Intermediates
25 Jun 2024 | Contributor(s):: Cardinal-David, Benoit, Harper, Kaid C., Verma, Anuj, Hanna, David, Caspi, Daniel D., Vitale, Christopher, Bien, Jeffrey T., Wang, Zhe, Diwan, Moiz
Manufacturing API and pharmaceutical intermediates requires the development of scalable, safe, and environmentally friendly processes. Reactions with high exothermicity or otherwise hazardous in nature, as well as reactions involving the formation of unstable intermediates, can benefit from...