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• Solvents and Organic Chemicals Organic Compounds Organoheterocyclic compounds Quinolines and derivatives Haloquinolines

Recent Advances in the Application of 4-Bromo-7-fluoro-quinoline (CAS: 1070879-29-6) in Chemical Biology and Pharmaceutical Research

The compound 4-bromo-7-fluoro-quinoline (CAS: 1070879-29-6) has recently emerged as a key intermediate in the synthesis of novel bioactive molecules, particularly in the fields of oncology and infectious disease research. This heterocyclic scaffold has garnered significant attention due to its versatile reactivity and ability to modulate various biological targets. Recent studies have highlighted its potential as a building block for kinase inhibitors and antimicrobial agents, with several research groups reporting promising results in preclinical models.

A 2023 study published in the Journal of Medicinal Chemistry demonstrated the utility of 4-bromo-7-fluoro-quinoline in developing selective JAK2 inhibitors. The bromo-fluoro substitution pattern was found to significantly enhance binding affinity while maintaining favorable pharmacokinetic properties. Researchers utilized this compound as a starting material for parallel synthesis, generating a library of 47 analogs with varying substitution patterns at the 4-position. Lead compounds showed nanomolar potency against JAK2 with >100-fold selectivity over other JAK isoforms.

In antimicrobial applications, a team at the University of Cambridge reported in Bioorganic & Medicinal Chemistry Letters the development of novel quinolone-antibiotic hybrids using 4-bromo-7-fluoro-quinoline as the core structure. The electron-withdrawing effects of the bromo and fluoro substituents were crucial for maintaining stability against bacterial efflux pumps. These hybrids demonstrated potent activity against multidrug-resistant Staphylococcus aureus strains (MIC values ranging from 0.25-2 μg/mL), with reduced cytotoxicity compared to existing fluoroquinolone antibiotics.

The synthetic accessibility of 4-bromo-7-fluoro-quinoline has also enabled its use in PROTAC (proteolysis targeting chimera) development. A Nature Chemical Biology publication detailed its incorporation into CRBN-recruiting PROTACs targeting BET proteins. The bromine atom served as an ideal handle for subsequent functionalization through Buchwald-Hartwig amination or Suzuki coupling, while the fluorine atom improved membrane permeability. These PROTAC molecules achieved >90% degradation of BRD4 at concentrations as low as 10 nM in cellular assays.

Recent advances in analytical characterization have provided deeper insights into the physicochemical properties of 4-bromo-7-fluoro-quinoline. A comprehensive study employing DFT calculations and X-ray crystallography revealed unexpected conformational preferences that influence its molecular recognition properties. These findings, published in ACS Omega, are guiding rational design approaches for new derivatives with optimized target engagement.

Looking forward, the unique properties of 4-bromo-7-fluoro-quinoline position it as a valuable scaffold for addressing emerging challenges in drug discovery, particularly in the development of targeted therapies and overcoming antibiotic resistance. Several pharmaceutical companies have included derivatives of this compound in their preclinical pipelines, suggesting its continued importance in medicinal chemistry research. Future directions likely include exploration of its applications in covalent inhibitor design and as a fluorescent probe for biological imaging.

• 1094754-90-1(3-Bromo-6-fluoro-1H-indole)
• 885520-70-7(4-Bromo-6-fluoro-1H-indole)
• 225366-90-5(3-bromo-7-fluoroquinoline)
• 927800-38-2(4-Bromo-8-fluoroquinoline)
• 661463-17-8(4-Bromo-6-fluoroquinoline)
• 885520-59-2(6-Bromo-4-fluoro-1H-indole)
• 1133115-78-2(5-Bromo-8-fluoroquinoline)
• 127827-52-5(6-Bromo-7-fluoroquinoline)
• 1416440-63-5(5-bromo-3-fluoro-quinoline)
• 1375108-29-4(7-bromo-3-fluoro-quinoline)