Work

Decagram-Scale Synthesis of the Novel Bacterial Topoisomerase Inhibitor OSUAB-0284

Year: 2025

Type: article

Abstract: Medicinal chemistry efforts identified OSUAB-0284 ( 2 ) as a preclinical candidate to treat staphylococcal infections, especially those caused by methicillin-resistant Staphylococcus aureus (MRSA). Herein, we describe a fit-for-purpose route that enabled the production of >20 g of API for toxicology studies and further preclinical characterization. Process improvements include a 16-fold increase in yield over the longest sequence, a 21-fold increase in efficiency for the cost-limiting reagent, and reduction of chromatography to one silica plug across an 18-step route.

Source: Organic Process Research & Development

DOI: 10.1021/acs.oprd.5c00033

Authors: Jason S. West, Chelsea A. Mann, Mark J. Mitton-Fry

Institution: The Ohio State University

Language: English

Topic: Chemical Synthesis and Analysis

Subfield: Molecular Biology

Field: Biochemistry, Genetics and Molecular Biology

Domain: Life Sciences

SDG: Good health and well-being

Open Access status: hybrid

Estimated APC paid: $4,500