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
PY - 2024/6/19
Y1 - 2024/6/19
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 - Pyrazoles/chemistry
KW - Pseudomonas aeruginosa/drug effects
KW - Anti-Bacterial Agents/pharmacology
KW - Biofilms/drug effects
KW - Humans
KW - Pseudomonas Infections/drug therapy
KW - Risk Assessment
UR - http://www.scopus.com/inward/record.url?scp=85197119622&partnerID=8YFLogxK
U2 - 10.3390/ijms25126737
DO - 10.3390/ijms25126737
M3 - Journal article
C2 - 38928443
SN - 1661-6596
VL - 25
JO - International Journal of Molecular Sciences
JF - International Journal of Molecular Sciences
IS - 12
M1 - 6737
ER -