Upscaling and Risk Evaluation of the Synthesis of the 3-5-diamino-1h-pyrazole, Disperazol
International Journal of Molecular Sciences(2024)
Abstract
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 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 active compound E, as performed by Fauske and Associates, LLC, Burr Ridge, IL, USA.
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Key words
biofilm,dispersal,pyrazole,c-di-GMP,large-scale synthesis,flow chemistry,safety,dust analysis,Pseudomonas aeruginosa,preclinical
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