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

Autor: Jansen CU; Department of Chemistry, Technical University of Denmark, DK-2800 Lyngby, Denmark., Grier KE; Department of Chemistry, Technical University of Denmark, DK-2800 Lyngby, Denmark., Andersen JB; Costerton Biofilm Center, Department of Immunology and Microbiology, Faculty of Health and Medical Sciences, University of Copenhagen, DK-2200 Copenhagen, Denmark., Hultqvist LD; Costerton Biofilm Center, Department of Immunology and Microbiology, Faculty of Health and Medical Sciences, University of Copenhagen, DK-2200 Copenhagen, Denmark., Nilsson M; Department of Odontology, University of Copenhagen, DK-2200 Copenhagen, Denmark., Moser C; Costerton Biofilm Center, Department of Immunology and Microbiology, Faculty of Health and Medical Sciences, University of Copenhagen, DK-2200 Copenhagen, Denmark.; Department of Clinical Microbiology, Copenhagen University Hospital, Rigshospitalet, DK-2100 Copenhagen, Denmark., Graz M; Costerton Biofilm Center, Department of Immunology and Microbiology, Faculty of Health and Medical Sciences, University of Copenhagen, DK-2200 Copenhagen, Denmark., Tolker-Nielsen T; Costerton Biofilm Center, Department of Immunology and Microbiology, Faculty of Health and Medical Sciences, University of Copenhagen, DK-2200 Copenhagen, Denmark., Givskov M; Costerton Biofilm Center, Department of Immunology and Microbiology, Faculty of Health and Medical Sciences, University of Copenhagen, DK-2200 Copenhagen, Denmark., Qvortrup K; Department of Chemistry, Technical University of Denmark, DK-2800 Lyngby, Denmark.
Jazyk: angličtina
Zdroj: International journal of molecular sciences [Int J Mol Sci] 2024 Jun 19; Vol. 25 (12). Date of Electronic Publication: 2024 Jun 19.
DOI: 10.3390/ijms25126737
Abstrakt: 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.
Databáze: MEDLINE
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