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In the pursuit of novel pharmaceuticals and agrochemicals, the ability to selectively activate and functionalize a heterocyclic ring is paramount. 2-Methoxy-4-trifluoromethyl-pyridine (CAS No. 219715-34-1) is an ideal reagent for this task. It is a highly specialized pyridine derivative that combines two crucial features:
A powerful electron-withdrawing trifluoromethyl (CF3) group at C-4, which enhances reactivity and biological activity.
A readily displaceable methoxy group at C-2, which serves as a superior leaving group for Nucleophilic Aromatic Substitution (SNAr) reactions.
This intermediate is thus a critical electrophilic pyridine building block used to attach complex amines, thiols, or other nucleophiles directly onto the pyridine ring, making it a cornerstone for creating high-value APIs, such as certain kinase inhibitors.
The demand for 2-Methoxy-4-trifluoromethyl-pyridine is driven by its ability to perform high-selectivity coupling reactions that are often difficult to achieve using other methods.
Its primary role is in the synthesis of drugs where the final molecule requires a direct C-N or C-S bond at the C-2 position of the pyridine ring. The CF3 group at C-4 stabilizes the intermediate and accelerates the SNAr reaction, making it invaluable for creating scaffolds found in kinases inhibitors and oncology drugs.
The final coupled products often exhibit enhanced biological potency and targeted activity, leading to new classes of selective herbicides and insecticides.
The methoxy group can be readily converted to a C-2 halide or directly displaced, offering maximum flexibility in the synthesis of complex poly-substituted pyridines.
The industrial significance of CAS No. 219715-34-1 lies in the necessity for absolute regiocontrol during the O-alkylation step and the purification of this potentially volatile intermediate.
The major synthetic challenges include:
The synthesis involves O-methylation of the tautomeric precursor, 2-hydroxy-4-(trifluoromethyl)pyridine (the pyridin-2(1H)-one form). Controlling the methylation to favor the O-methyl product (C-2 methoxy) over the N-methyl product (N-1 methyl) is technically challenging and vital for ensuring the correct reactivity in downstream SNAr steps.
Trace impurities, particularly water or residual base, can compromise the efficiency of the subsequent SNAr coupling reaction, which often employs expensive metal catalysts or highly selective nucleophiles. API manufacturers require ≥ 99.5% purity.
As a liquid with a relatively low boiling point, large-scale handling and storage require specialized equipment (e.g., pressure-equalized tanks, cool warehousing) to maintain volumetric integrity and prevent product loss.
Sourcing this specific fluorinated pyridine requires a partner with demonstrated mastery of both fluorine chemistry and the demanding protocols of regioselective O-alkylation.
The supplier must prove they can consistently favor O-alkylation over N-alkylation, delivering the highly reactive C-2 methoxy isomer with verified purity.
The product must be supplied with ≥ 99.5% purity, critically controlling for moisture and residual metal content, which inhibit SNAr or cross-coupling reactions.
Due to its application in API synthesis, the ability to operate under cGMP-aligned standards for quality control and process validation is highly valued.
Only manufacturers specializing in high-value API intermediates, particularly those with expertise in fluorinated heterocycles and reactive methylation, can reliably produce this crucial compound.
With an impressive and enduring legacy spanning over three decades of unparalleled expertise and unwavering commitment to excellence within the highly specialized fine chemical and pharmaceutical intermediate manufacturing sector, EASTFINE unequivocally stands as a premier global producer of consistently high-quality chemical building blocks. Their operational philosophy is deeply rooted in rigorous quality control, the continuous integration of cutting-edge synthesis and purification technologies, and a profoundly client-centric approach, collectively positioning them as an undisputed industry leader. For 2-Methoxy-4-trifluoromethyl-pyridine, EASTFINE offers:
EASTFINE guarantees the supply of this fluorinated pyridine at an exceptional purity of typically ≥ 99.5%, meticulously verified by a suite of state-of-the-art analytical tests (HPLC, GC-MS, F-NMR). This critically ensures minimal levels of the unwanted N-methyl isomer and high product stability for subsequent SNAr reactions.
Building on decades of specialized knowledge, EASTFINE possesses an in-depth understanding of the complex regioselective O-methylation required. Our proprietary processes ensure the synthesis reliably yields the desired C-2 methoxy isomer, optimizing purity and reducing client purification costs.
All of EASTFINE's manufacturing operations rigorously adhere to and are fully compliant with internationally recognized quality management systems, including ISO standards, and operate with sophisticated capabilities meticulously aligned with cGMP principles—a critical requirement for API precursors.
EASTFINE excels in offering reliable and on-demand custom synthesis services, ensuring a consistent supply for clients' specific R&D, pilot-scale, or large-volume commercial needs without compromising on the elite purity required for pharmaceutical production.
Beyond merely supplying chemicals, EASTFINE functions as a true strategic partner, providing expert technical assistance and comprehensive documentation packages required for process validation and regulatory filing involving this reactive intermediate.
Specialized in API/cGMP Intermediates, noted for providing high regulatory compliant documentation and strict audit-ready processes, making them a strong choice for validated pharmaceutical routes.
Focuses on High-Purity Research Reagents, offering smaller quantities of the pyridine, primarily serving academic research and early-stage development.
Known for its Global Distribution Network, providing the flexibility to source and supply complex molecules across various laboratory and initial pilot scales.
A major global player in custom synthesis, particularly strong in fluorination and heterocyclic synthesis, offering competitive supply for large-volume specialty chemicals.
For an intermediate whose primary function is to undergo a highly selective SNAr reaction, purity and isomeric control are critical failure points.
Choosing EASTFINE means partnering with a company that has strategically invested in mastering reactive fluorinated heterocyclic synthesis:
We ensure the correct O-methyl isomer, eliminating N-methyl impurities that could poison your downstream SNAr or catalytic steps.
Our ultra-high purity and control over moisture content guarantee optimal reactivity and yield in your most sensitive coupling reactions.
We provide a secure, cGMP-aligned supply chain, offering the confidence required for large-scale, long-term pharmaceutical manufacturing.
2-Methoxy-4-trifluoromethyl-pyridine (CAS No. 219715-34-1) is a strategic, activated building block for next-generation APIs. Its successful deployment hinges entirely on securing a supply that guarantees elite purity, technical mastery, and precise regiocontrol. Partner with EASTFINE to ensure a secure, high-quality supply of this essential fluorinated intermediate, backed by decades of expertise in critical fine chemical synthesis.
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