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The Application of a Continuous Grignard Reaction in the Preparation of Fluconazole
10 May 2024 | Contributor(s):: Korwar, Sudha, Amir, Somi, Tosso, Perrer N., Desai, Bimbisar K., Kong, Caleb J., Fadnis, Swara, Telang, Nakul S., Ahmad, Saeed, Roper, Thomas D., Gupton, B. Frank
The application of continuous methods in the synthesis of active pharmaceutical ingredients continues to receive significant attention in the academic as well as the industrial research communities. One of the major advantages of continuous methods is the ability to safely access kinetic synthons...
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Automated and continuous synthesis of drug substances
Peer-reviewed journal | 24 Apr 2024 | Contributor(s):: Sacher, Stephan, Castillo, Ismael, Rehrl, Jakob, Sagmeister, Peter, Lebl, René, Kruisz, Julia, Celikovic, Selma, Sipek, Martin, Williams, Jason D., Kirschneck, Dirk, Kappe, C. Oliver, Horn, Martin
A continuous synthesis line was developed integrating different common reaction steps namely nitration, substitution and hydrogenation. Mesalazine as model drug substance was produced from 2-chlorobenzoic acid in continuous flow mode. A multi-instrument PAT strategy was implemented to equip the...
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An expeditious synthesis of imatinib and analogues utilising flow chemistry methods
Peer-reviewed journal | 24 Apr 2024 | Contributor(s):: Hopkin, Mark D., Baxendale, Ian R., Ley, Steven V.
A flow-based route to imatinib, the API of Gleevec, was developed and the general procedure then used to generate a number of analogues which were screened for biological activity against Abl1. The flow synthesis required minimal manual intervention and was achieved despite the poor solubility of...
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Rapid On-Demand Synthesis of Lomustine under Continuous Flow Conditions
Peer-reviewed journal | 09 Jun 2023 | Contributor(s):: Jaman, Z, Sobreira, TJPMufti, A, Ferreira, CR, Cooks, RG, Thompson, DH
Lomustine, an important agent for treatment of brain tumors and Hodgkin's lymphoma, has been synthesized using continuous flow methodology. Desorption electrospray ionization mass spectrometry (DESI-MS) was used to quickly explore a large number of reaction conditions for one of the reaction...