Upscaling and Risk Evaluation of the Synthesis of the 3,5-Diamino-1H-Pyrazole, Disperazol
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Upscaling and Risk Evaluation of the Synthesis of the 3,5-Diamino-1H-Pyrazole, Disperazol. / 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.
In: International Journal of Molecular Sciences, Vol. 25, No. 12, 6737, 2024.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - Upscaling and Risk Evaluation of the Synthesis of the 3,5-Diamino-1H-Pyrazole, Disperazol
AU - Jansen, Charlotte Uldahl
AU - Grier, Katja Egeskov
AU - Andersen, Jens Bo
AU - Hultqvist, Louise Dahl
AU - Nilsson, Martin
AU - Moser, Claus
AU - Graz, Michael
AU - Tolker-Nielsen, Tim
AU - Givskov, Michael
AU - Qvortrup, Katrine
N1 - Publisher Copyright: © 2024 by the authors.
PY - 2024
Y1 - 2024
N2 - 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.
AB - 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.
KW - biofilm
KW - c-di-GMP
KW - dispersal
KW - dust analysis
KW - flow chemistry
KW - large-scale synthesis
KW - preclinical
KW - Pseudomonas aeruginosa
KW - pyrazole
KW - safety
U2 - 10.3390/ijms25126737
DO - 10.3390/ijms25126737
M3 - Journal article
C2 - 38928443
AN - SCOPUS:85197119622
VL - 25
JO - International Journal of Molecular Sciences (Online)
JF - International Journal of Molecular Sciences (Online)
SN - 1661-6596
IS - 12
M1 - 6737
ER -
ID: 398072077