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• Solvents and Organic Chemicals Organic Compounds Organoheterocyclic compounds Benzopyrazoles Indazoles
• Solvents and Organic Chemicals Organic Compounds Heterocyclic Compounds

Research Brief on 5-Fluoro-1H-indazole-3-carboxylic acid (CAS: 1077-96-9): Recent Advances and Applications

5-Fluoro-1H-indazole-3-carboxylic acid (CAS: 1077-96-9) is a fluorinated indazole derivative that has garnered significant attention in the field of medicinal chemistry due to its versatile applications as a building block for pharmaceuticals and bioactive compounds. Recent studies have highlighted its potential in the development of kinase inhibitors, anti-inflammatory agents, and anticancer therapeutics. This research brief synthesizes the latest findings on this compound, focusing on its synthesis, biological activity, and emerging applications in drug discovery.

A 2023 study published in the Journal of Medicinal Chemistry demonstrated the efficacy of 5-Fluoro-1H-indazole-3-carboxylic acid as a key intermediate in the synthesis of novel Bruton's tyrosine kinase (BTK) inhibitors. The researchers utilized a microwave-assisted synthetic route to optimize the yield and purity of the compound, achieving a scalable process suitable for industrial applications. The resulting BTK inhibitors exhibited potent activity against B-cell malignancies, with IC50 values in the nanomolar range.

In the realm of anti-inflammatory drug development, a recent patent application (WO2023056789) disclosed the use of 5-Fluoro-1H-indazole-3-carboxylic acid derivatives as selective COX-2 inhibitors. The lead compound from this series showed superior gastrointestinal safety profiles compared to traditional NSAIDs, making it a promising candidate for chronic inflammatory conditions. Molecular docking studies revealed that the fluorine atom at the 5-position enhances binding affinity to the COX-2 active site through favorable hydrophobic interactions.

Advancements in structural modification strategies have expanded the utility of this scaffold. A 2024 paper in Bioorganic & Medicinal Chemistry Letters reported the development of 5-Fluoro-1H-indazole-3-carboxylic acid-based PROTACs (Proteolysis Targeting Chimeras) targeting estrogen receptor alpha (ERα) for breast cancer therapy. The bifunctional molecules effectively induced ERα degradation in MCF-7 cells, demonstrating the compound's adaptability in modern drug discovery platforms.

From a safety perspective, recent toxicological assessments (Regulatory Toxicology and Pharmacology, 2023) have established favorable ADME profiles for 5-Fluoro-1H-indazole-3-carboxylic acid derivatives. The compounds showed good metabolic stability in human liver microsomes and minimal inhibition of major CYP450 isoforms, addressing potential drug-drug interaction concerns. These findings support further preclinical development of therapeutics based on this chemical scaffold.

The commercial availability of 5-Fluoro-1H-indazole-3-carboxylic acid from multiple suppliers (purity ≥98%) has facilitated its widespread adoption in research. Current market analysis indicates growing demand, with projected compound annual growth rate (CAGR) of 7.2% from 2024 to 2030, driven by increasing applications in targeted cancer therapies and immunomodulators. Several pharmaceutical companies have included derivatives of this compound in their early-stage pipelines.

Future research directions include exploring the compound's potential in combination therapies and its application in radiopharmaceuticals. The presence of the fluorine atom offers opportunities for ¹⁸F labeling, making it attractive for PET imaging probe development. Collaborative efforts between academic institutions and pharmaceutical companies are expected to accelerate the translation of these findings into clinical applications in the coming years.

• 4498-67-3(Indazole-3-carboxylic acid)
• 885279-26-5(Methyl 6-fluoro-1H-indazole-3-carboxylate)
• 129295-33-6(5,6-difluoro-2H-indazole-3-carboxylic acid)
• 959236-59-0(7-Fluoro-1H-indazole-3-carboxylic acid)
• 1201-24-7(5-Methyl-1h-indazole-3-carboxylic acid)
• 78155-73-4(Methyl 5-fluoro-1H-indazole-3-carboxylate)
• 1016-36-0(Ethyl 5-fluoro-1H-indazole-3-carboxylate)
• 885518-90-1(4-Methyl-1H-indazole-3-carboxylic acid)
• 885523-11-5(4,6-Difluoro-1H-indazole-3-carboxylic acid)
• 885521-64-2(4-Fluoro-1H-indazole-3-carboxylic acid)