Upscaling and Risk Evaluation of the Synthesis of the 3,5-Diamino-1H-Pyrazole, Disperazol-Reference-Cited by-同舟云学术

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

Published:2024-06-19 Issue:12 Volume:25 Page:6737
ISSN:1422-0067
Container-title:International Journal of Molecular Sciences
language:en
Short-container-title:IJMS

Author:

Jansen Charlotte Uldahl¹^ORCID,Grier Katja Egeskov¹^ORCID,Andersen Jens Bo²^ORCID,Hultqvist Louise Dahl²^ORCID,Nilsson Martin³^ORCID,Moser Claus²⁴,Graz Michael²,Tolker-Nielsen Tim²,Givskov Michael²,Qvortrup Katrine¹

Affiliation:

1. Department of Chemistry, Technical University of Denmark, DK-2800 Lyngby, Denmark

2. Costerton Biofilm Center, Department of Immunology and Microbiology, Faculty of Health and Medical Sciences, University of Copenhagen, DK-2200 Copenhagen, Denmark

3. Department of Odontology, University of Copenhagen, DK-2200 Copenhagen, Denmark

4. Department of Clinical Microbiology, Copenhagen University Hospital, Rigshospitalet, DK-2100 Copenhagen, Denmark

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.

Funder

Sygeforsikringen

Publisher

MDPI AG

Link

https://www.mdpi.com/1422-0067/25/12/6737/pdf

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