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3,5-二氨基-1H-吡唑、迪斯帕唑的合成放大及风险评估。

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

机构信息

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

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

出版信息

Int J Mol Sci. 2024 Jun 19;25(12):6737. doi: 10.3390/ijms25126737.

DOI:10.3390/ijms25126737
PMID:38928443
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11203405/
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 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 , as performed by Fauske and Associates, LLC, Burr Ridge, IL, USA.

摘要

本文介绍了将实验室规模的合成（1 克）转化为大规模（400 克）合成 3-5-二氨基-1H-吡唑 Disperazol 的工作，这是一种用于治疗抗生素耐药生物膜感染的新型药物。实验室规模合成中潜在危险的重氮化步骤转化为安全且易于处理的流动化学步骤。此外，本文还介绍了 Fauske and Associates，LLC（美国伊利诺伊州伯里奇）对活性化合物进行的 OSHA 推荐的安全评估。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/645c/11203405/6b5fd83e6be9/ijms-25-06737-sch005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/645c/11203405/04a00e20d6bc/ijms-25-06737-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/645c/11203405/5daed9c5c797/ijms-25-06737-sch002.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/645c/11203405/6b5fd83e6be9/ijms-25-06737-sch005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/645c/11203405/04a00e20d6bc/ijms-25-06737-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/645c/11203405/5daed9c5c797/ijms-25-06737-sch002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/645c/11203405/ce3f343459cb/ijms-25-06737-sch003.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/645c/11203405/6b5fd83e6be9/ijms-25-06737-sch005.jpg

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