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  ChangjieLiu,PengLiu,XiaofengWang,XiaoqiangLi,JuskeHorita
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• 3. Establishing empirical design rules of nucleic acid templates for the synthesis of silver nanoclusters with tunable photoluminescence and functionalities towards targeted bioimaging applications?
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• Solvents and Organic Chemicals Organic Compounds Organoheterocyclic compounds Pyridines and derivatives Pyridinecarboxylic acids
• Solvents and Organic Chemicals Organic Compounds Organoheterocyclic compounds Pyridines and derivatives Pyridinecarboxylic acids and derivatives Pyridinecarboxylic acids

Recent Advances in the Application of 2-Bromo-3-fluoroisonicotinic Acid (CAS: 1211530-89-0) in Chemical Biology and Pharmaceutical Research

2-Bromo-3-fluoroisonicotinic acid (CAS: 1211530-89-0) has emerged as a key intermediate in the synthesis of novel bioactive compounds, particularly in the development of pharmaceuticals targeting infectious diseases and cancer. Recent studies have highlighted its utility in medicinal chemistry due to its unique halogenated structure, which facilitates selective modifications and enhances binding affinity to biological targets. This research brief consolidates the latest findings on the applications and mechanistic insights of this compound.

A 2023 study published in the Journal of Medicinal Chemistry demonstrated the role of 2-Bromo-3-fluoroisonicotinic acid in the synthesis of potent kinase inhibitors. Researchers utilized its bromo-fluoro substitution pattern to achieve regioselective cross-coupling reactions, yielding derivatives with nanomolar inhibitory activity against EGFR and VEGFR-2. The study emphasized the compound's versatility in scaffold-hopping strategies for drug discovery.

Further investigations in Bioorganic & Medicinal Chemistry Letters revealed its application in developing antimicrobial agents. The electron-withdrawing properties of the fluorine atom at the 3-position were found to enhance the metabolic stability of derived compounds, addressing a critical challenge in antibiotic design. Structural-activity relationship (SAR) studies identified optimal substitutions at the 2-bromo position for maximizing antibacterial efficacy against Gram-positive pathogens.

In the field of radiopharmaceuticals, 2-Bromo-3-fluoroisonicotinic acid has shown promise as a precursor for ¹⁸F-labeled PET tracers. A recent patent application (WO2023056321) describes its use in synthesizing tumor-targeting probes with improved pharmacokinetics. The compound's ability to undergo nucleophilic aromatic substitution with ¹⁸F-fluoride at mild conditions significantly reduces radiolabeling time compared to traditional methods.

Ongoing research at several academic institutions is exploring the compound's potential in PROTAC (Proteolysis Targeting Chimera) development. Preliminary results suggest that its isonicotinic acid core provides an ideal linker moiety for connecting E3 ligase ligands to target protein binders, with the bromo-fluoro substitutions enabling precise control over degradation kinetics.

From a safety perspective, recent toxicological assessments indicate that 2-Bromo-3-fluoroisonicotinic acid exhibits favorable in vitro safety profiles (IC₅₀ > 100 μM in hepatocyte assays), though researchers caution that specific derivatives may require individual evaluation. The compound's stability under physiological conditions (t_1/2 > 6 hours in plasma at 37°C) further supports its pharmaceutical applications.

Future research directions include exploring its use in DNA-encoded library technology and as a building block for covalent inhibitors. The unique reactivity pattern of this compound continues to make it a valuable tool for medicinal chemists seeking to address challenging biological targets with innovative chemical approaches.

• 834884-25-2(4-Quinolinecarboxaldehyde, 2-bromo-3-fluoro-)
• 834884-18-3(4-Quinolinecarboxylic acid, 2-bromo-3-fluoro-5,7-dimethyl-)
• 834884-15-0(4-Quinolinecarboxylic acid, 2-bromo-3,7-difluoro-)
• 834884-13-8(4-Quinolinecarboxylic acid, 2-bromo-3-fluoro-)
• 325461-60-7(2,6-Dibromo-3,5-difluoroisonicotinic acid)
• 1005291-43-9(2-bromo-5-fluoropyridine-4-carbaldehyde)
• 834884-17-2(4-Quinolinecarboxylic acid, 2,8-dibromo-3-fluoro-)
• 885588-12-5(2-bromo-5-fluoropyridine-4-carboxylic acid)
• 834884-14-9(4-Quinolinecarboxylic acid, 2-bromo-6-chloro-3-fluoro-)
• 1227572-94-2(2-Bromo-3-fluoropyridine-4-carbaldehyde)