open access publication

Article, 2024

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

International Journal of Molecular Sciences, ISSN 1661-6596, 1422-0067, Volume 25, 12, Page 6737, 10.3390/ijms25126737

Contributors

Jansen, Charlotte Uldahl 0000-0002-1168-8002 [1] Grier, Katja Egeskov 0000-0002-9854-1440 [1] Andersen, Jens Bo 0000-0003-1720-1581 [2] Hultqvist, Louise Dahl 0000-0003-0256-892X [2] Nilsson, Martin 0000-0001-6251-9842 [2] Moser, Claus Ernst 0000-0002-7664-8570 [2] [3] Graz, Michael [2] Tolker-Nielsen, Tim 0000-0002-9751-474X [2] Givskov, Michael [2] Qvortrup, Katrine M 0000-0003-3828-2069 (Corresponding author) [1]

Affiliations

  1. [1] Technical University of Denmark
  2. [NORA names: DTU Technical University of Denmark; University; Denmark; Europe, EU; Nordic; OECD];
  3. [2] University of Copenhagen
  4. [NORA names: KU University of Copenhagen; University; Denmark; Europe, EU; Nordic; OECD];
  5. [3] Rigshospitalet
  6. [NORA names: Capital Region of Denmark; Hospital; Denmark; Europe, EU; Nordic; OECD]

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.

Keywords

Fauske, IL, LLC, USA, association, biofilm infections, burr, chemistry step, evaluation, infection, lab-scale synthesis, large-scale, pharmaceuticals, ridge, risk, risk evaluation, steps, synthesis, treatment, upscaling

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