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

This paper presents the work performed to transition a 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 biofilm infections. The potentially hazardous diazotisation step in the lab-scale...

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Bibliographic Details
Published in:International journal of molecular sciences 2024-06, Vol.25 (12), p.6737
Main Authors: Jansen, Charlotte Uldahl, Grier, Katja Egeskov, Andersen, Jens Bo, Hultqvist, Louise Dahl, Nilsson, Martin, Moser, Claus, Graz, Michael, Tolker-Nielsen, Tim, Givskov, Michael, Qvortrup, Katrine
Format: Article
Language:English
Subjects:
Anti-Bacterial Agents - chemical synthesis
Anti-Bacterial Agents - chemistry
Anti-Bacterial Agents - pharmacology
Bacterial infections
Biofilms - drug effects
Care and treatment
Chemistry
Decomposition
Dust
Electrical codes
Friction
Heat
Humans
Pseudomonas aeruginosa - drug effects
Pseudomonas Infections - drug therapy
Pseudomonas Infections - microbiology
Pyrazoles - chemical synthesis
Pyrazoles - chemistry
Pyrazoles - pharmacology
Reagents
Risk Assessment
Temperature
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Summary:This paper presents the work performed to transition a 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 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 active compound , as performed by Fauske and Associates, LLC, Burr Ridge, IL, USA.
ISSN:1422-0067
1661-6596
1422-0067
DOI:10.3390/ijms25126737