Upscaling and Risk Evaluation of the Synthesis of the 3-5-Diamino-1H-Pyrazole, Disperazol

Charlotte Uldahl Jansen; Katja Egeskov Grier; Jens Bo Andersen; Louise Dahl Hultqvist; Martin Nilsson; Claus Moser; Michael Graz; Tim Tolker-Nielsen; Michael Givskov; Katrine Qvortrup

doi:10.20944/preprints202405.1657.v1

How to cite: Jansen, C. U.; Grier, K. E.; Andersen, J. B.; Hultqvist, L. D.; Nilsson, M.; Moser, C.; Graz, M.; Tolker-Nielsen, T.; Givskov, M.; Qvortrup, K. Upscaling and Risk Evaluation of the Synthesis of the 3-5-Diamino-1H-Pyrazole, Disperazol. Preprints 2024, 2024051657. https://doi.org/10.20944/preprints202405.1657.v1 Jansen, C. U.; Grier, K. E.; Andersen, J. B.; Hultqvist, L. D.; Nilsson, M.; Moser, C.; Graz, M.; Tolker-Nielsen, T.; Givskov, M.; Qvortrup, K. Upscaling and Risk Evaluation of the Synthesis of the 3-5-Diamino-1H-Pyrazole, Disperazol. Preprints 2024, 2024051657. https://doi.org/10.20944/preprints202405.1657.v1

Abstract

This paper presents the work done to transition the lab scale synthesis (1 g) to a large scale (400 g) synthesis of the 3-5-diamino-1H-Pyrazole Disperazol; a new pharmaceutical for treatment of antibiotic resistant Pseudomonas aeruginosa biofilm infections. The potentially hazardous diazotisation step in the lab scale synthesis was transformed to a safe and easy to handle flow chemistry step. Additionally, the paper presents an OSHA recommended safety assessment of the active compound E, performed by Fauske and Associates, LLC.

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Copyright: This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

Upscaling and Risk Evaluation of the Synthesis of the 3-5-Diamino-1H-Pyrazole, Disperazol

Abstract

Keywords

Subject

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