• 1. Evolved polymerases facilitate selection of fully 2′-OMe-modified aptamers?
  Zhixia Liu,Tingjian Chen,Floyd E. Romesberg Chem. Sci., 2017,8, 8179-8182
• 2. Evolution of calcium phosphate precipitation in hanging drop vapor diffusion by in situRaman microspectroscopy
  Gloria Belén Ramírez-Rodríguez,José Manuel Delgado-López,Jaime Gómez-Morales CrystEngComm, 2013,15, 2206-2212
• 3. Essential effect of the electrolyte on the mechanical and chemical degradation of LiNi0.8Co0.15Al0.05O2 cathodes upon long-term cycling??
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• Solvents and Organic Chemicals Organic Compounds Organoheterocyclic compounds Diazines Pyrimidines and pyrimidine derivatives Pyrimidinecarboxylic acids and derivatives

Recent Advances in the Study of 2-Methanesulfonyl-6-methylpyrimidine-4-carboxylic Acid (CAS: 1263216-10-9)

2-Methanesulfonyl-6-methylpyrimidine-4-carboxylic acid (CAS: 1263216-10-9) has recently emerged as a compound of significant interest in the field of chemical biology and pharmaceutical research. This pyrimidine derivative has shown promising potential in various therapeutic applications, particularly as a key intermediate in the synthesis of novel drug candidates. Recent studies have focused on its structural properties, synthetic pathways, and biological activities, shedding light on its mechanism of action and potential clinical applications.

The compound's unique chemical structure, featuring a methanesulfonyl group and a carboxylic acid moiety, has been the subject of extensive investigation. Researchers have explored its role as a building block for the development of kinase inhibitors, which are crucial in targeting various signaling pathways involved in cancer and inflammatory diseases. A 2023 study published in the Journal of Medicinal Chemistry demonstrated the compound's efficacy in the synthesis of selective JAK2 inhibitors, showing promising results in preclinical models of myeloproliferative disorders.

Recent synthetic methodologies have focused on optimizing the production of 2-methanesulfonyl-6-methylpyrimidine-4-carboxylic acid with improved yield and purity. A team at MIT developed a novel catalytic system in 2024 that reduces byproduct formation during the sulfonylation step, achieving a 92% yield compared to traditional methods' 65-70%. This advancement has significant implications for scaling up production while maintaining cost-effectiveness, a critical factor in pharmaceutical development.

Biological evaluations have revealed interesting pharmacokinetic properties of derivatives based on this scaffold. The compound's moderate lipophilicity (logP ~1.8) and good aqueous solubility (>10 mg/mL at pH 7.4) make it particularly suitable for oral drug formulations. Recent in vivo studies conducted by Pfizer researchers demonstrated that analogs containing this core structure exhibited favorable bioavailability profiles in rodent models, with plasma concentrations reaching therapeutic levels within 2 hours post-administration.

The safety profile of 2-methanesulfonyl-6-methylpyrimidine-4-carboxylic acid and its derivatives has been another area of active research. Toxicology studies published in Regulatory Toxicology and Pharmacology (2024) indicated that the compound shows minimal off-target effects at therapeutic doses, with no observed hepatotoxicity or cardiotoxicity in animal models. These findings support its potential as a safe scaffold for further drug development.

Looking forward, several pharmaceutical companies have included derivatives of 2-methanesulfonyl-6-methylpyrimidine-4-carboxylic acid in their preclinical pipelines. The compound's versatility as a synthetic intermediate and its favorable physicochemical properties position it as a valuable asset in medicinal chemistry. Ongoing research is exploring its application in developing treatments for autoimmune disorders, with Phase I clinical trials expected to begin in late 2025 for a rheumatoid arthritis candidate based on this chemical scaffold.

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