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  Suji Lee,Min Su Han Chem. Commun., 2021,57, 9450-9453
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Recent Advances in the Study of 2-Tert-butylpyrimidin-4-amine (CAS: 114362-20-8) in Chemical Biology and Pharmaceutical Research

The compound 2-Tert-butylpyrimidin-4-amine (CAS: 114362-20-8) has recently garnered significant attention in the field of chemical biology and pharmaceutical research due to its potential applications in drug discovery and development. This heterocyclic amine, characterized by a pyrimidine core with a tert-butyl substituent, has been explored for its unique chemical properties and biological activities. Recent studies have focused on its role as a building block in the synthesis of novel bioactive molecules, particularly in the context of kinase inhibition and targeted cancer therapies.

One of the most notable advancements in the study of 2-Tert-butylpyrimidin-4-amine is its incorporation into small-molecule inhibitors targeting protein kinases. Kinases play a critical role in cellular signaling pathways, and their dysregulation is often associated with various diseases, including cancer. Researchers have synthesized derivatives of 2-Tert-butylpyrimidin-4-amine to enhance their selectivity and potency against specific kinase targets. For instance, a 2023 study published in the Journal of Medicinal Chemistry demonstrated that modifications to the pyrimidine scaffold significantly improved the compound's inhibitory activity against EGFR (epidermal growth factor receptor) mutants, which are implicated in non-small cell lung cancer.

In addition to its applications in oncology, 2-Tert-butylpyrimidin-4-amine has also been investigated for its potential in anti-inflammatory and antimicrobial therapies. A recent preprint on bioRxiv highlighted its role as a precursor in the synthesis of compounds with dual activity against bacterial pathogens and inflammatory cytokines. The study reported that derivatives of 2-Tert-butylpyrimidin-4-amine exhibited promising in vitro activity against methicillin-resistant Staphylococcus aureus (MRSA) while also modulating the production of pro-inflammatory cytokines such as TNF-α and IL-6.

The synthetic accessibility of 2-Tert-butylpyrimidin-4-amine has further contributed to its popularity in medicinal chemistry. Researchers have developed efficient and scalable routes for its synthesis, enabling rapid exploration of its derivatives. A 2022 patent (US20220169678A1) disclosed a novel one-pot synthesis method that significantly reduces production costs and improves yield, making it more feasible for large-scale pharmaceutical applications. This methodological advancement is expected to accelerate the development of new drugs based on this scaffold.

Despite these promising developments, challenges remain in optimizing the pharmacokinetic properties of 2-Tert-butylpyrimidin-4-amine derivatives. Issues such as poor solubility and metabolic stability have been reported in preclinical studies. However, recent efforts in prodrug design and formulation technologies, such as nanoparticle encapsulation, have shown potential in overcoming these limitations. A 2023 study in Molecular Pharmaceutics demonstrated that a nanoparticle-formulated derivative of 2-Tert-butylpyrimidin-4-amine achieved enhanced bioavailability and tumor accumulation in murine models, paving the way for future clinical translation.

In conclusion, 2-Tert-butylpyrimidin-4-amine (CAS: 114362-20-8) represents a versatile and promising scaffold in chemical biology and pharmaceutical research. Its applications span from kinase inhibitors to antimicrobial agents, supported by ongoing advancements in synthetic methodologies and formulation technologies. Future research should focus on addressing its pharmacokinetic challenges and expanding its therapeutic potential through innovative drug design strategies.

• 10491-77-7(2-ethylpyrimidin-4-amine)
• 265324-26-3(2-Cyclopropylpyrimidin-4-amine)
• 134318-72-2(4-Amino-2-pyrimidineacetonitrile)
• 52698-68-7(2-Isopropyl-N-methylpyrimidin-4-amine)
• 67305-22-0(4,6-Pyrimidinediamine, 2-tricyclo[3.3.1.13,7]dec-1-yl-)
• 18202-78-3(2-(Tert-butyl)pyrimidine-4,5-diamine)
• 408352-57-8(4,6-Pyrimidinediamine,2-ethyl-)
• 114362-19-5(2-Isopropyl-pyrimidin-4-ylamine)
• 100910-69-8(4-Amino-2-(N-propyl)pyrimidine)
• 1483220-52-5(2-(2-methylcyclopropyl)pyrimidin-4-amine)