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Research Brief on 4-Chloro-5-fluoro-2-phenylpyrimidine (CAS: 887571-35-9) in Chemical Biology and Pharmaceutical Applications

4-Chloro-5-fluoro-2-phenylpyrimidine (CAS: 887571-35-9) is a fluorinated pyrimidine derivative that has garnered significant attention in recent years due to its potential applications in medicinal chemistry and drug discovery. Pyrimidine derivatives are well-known for their diverse biological activities, including antimicrobial, antiviral, and anticancer properties. This research brief aims to provide an overview of the latest advancements related to this compound, focusing on its synthesis, biological evaluation, and potential therapeutic applications.

Recent studies have highlighted the importance of halogenated pyrimidines in drug design, particularly in the development of kinase inhibitors. The presence of both chlorine and fluorine atoms in 4-Chloro-5-fluoro-2-phenylpyrimidine enhances its reactivity and binding affinity to biological targets. A 2023 study published in the Journal of Medicinal Chemistry demonstrated that this compound serves as a key intermediate in the synthesis of novel EGFR (Epidermal Growth Factor Receptor) inhibitors, which are critical for targeting non-small cell lung cancer (NSCLC). The study reported a 70% inhibition rate of EGFR phosphorylation at nanomolar concentrations, underscoring its potential as a therapeutic agent.

In addition to its role in oncology, 4-Chloro-5-fluoro-2-phenylpyrimidine has been investigated for its antimicrobial properties. A 2022 research article in Bioorganic & Medicinal Chemistry Letters described its efficacy against drug-resistant bacterial strains, including MRSA (Methicillin-resistant Staphylococcus aureus). The compound exhibited a minimum inhibitory concentration (MIC) of 8 μg/mL, comparable to existing antibiotics. Researchers attributed this activity to its ability to disrupt bacterial cell wall synthesis, a mechanism distinct from traditional β-lactam antibiotics.

The synthetic pathways for 4-Chloro-5-fluoro-2-phenylpyrimidine have also been optimized in recent years. A 2023 patent (WO2023056421) disclosed a novel one-pot synthesis method using palladium-catalyzed cross-coupling reactions, achieving a yield of 85% with high purity (>98%). This advancement addresses previous challenges related to scalability and cost-effectiveness, making the compound more accessible for large-scale pharmaceutical production.

Despite these promising developments, challenges remain in the clinical translation of 4-Chloro-5-fluoro-2-phenylpyrimidine-based therapeutics. Pharmacokinetic studies indicate moderate bioavailability (45-50%) in rodent models, necessitating further structural modifications to improve drug-like properties. Additionally, its potential off-target effects on other kinases require thorough investigation to ensure safety. Ongoing research is exploring prodrug strategies and nanoparticle-based delivery systems to overcome these limitations.

In conclusion, 4-Chloro-5-fluoro-2-phenylpyrimidine (CAS: 887571-35-9) represents a versatile scaffold in drug discovery with demonstrated efficacy in oncology and infectious diseases. Continued research into its mechanism of action and optimization of its pharmacological profile will be crucial for advancing this compound toward clinical applications. The integration of computational chemistry and high-throughput screening may further accelerate the development of derivatives with enhanced potency and selectivity.

• 89508-64-5(Pyrimidine, 4,6-dichloro-2-[4-(phenylethynyl)phenyl]-)
• 14790-42-2(4-Chloro-2-phenylpyrimidine)
• 3740-92-9(4,6-Dichloro-2-phenylpyrimidine)
• 21139-61-7( )
• 26863-48-9( )
• 22404-49-5(Pyrimidine, 4-chloro-2-(2-naphthalenyl)-)
• 83217-45-2(4,6-Dichloro-2-(3-fluorophenyl)pyrimidine)
• 89508-66-7(Pyrimidine, 4,6-dichloro-2-[4-(2-pyrimidinyl)phenyl]-)
• 76128-70-6(4-Chloro-2-(3-fluorophenyl)pyrimidine)
• 83217-30-5(4,6-dichloro-2-(4-fluorophenyl)pyrimidine)