Views: 0 Author: Site Editor Publish Time: 2026-01-15 Origin: Site
In 2026, the battle against Chronic Myeloid Leukemia (CML) and Gastrointestinal Stromal Tumors (GIST) has reached a high-tech plateau. While newer therapies emerge, Imatinib Mesylate remains the fundamental standard of care. This "magic bullet" drug relies entirely on the structural integrity of its precursors.
N-(5-nitro-2-methylphenyl)-4-(3-pyridyl)-2-pyrimidineamine (CAS No. 152460-09-8) is the most critical of these precursors. As a complex aromatic heterocycle, it contains the "pyrimidine-amine" bridge that is essential for the drug’s docking into the BCR-ABL kinase enzyme. Any impurity in this intermediate can lead to genotoxic contaminants in the final drug product, making the manufacturer's role vital to patient safety.
Following your request, we break down the critical facets of this molecule in the strictly required order.
This compound is a nitro-substituted aromatic pyrimidineamine. Structurally, it consists of a central pyrimidine ring substituted at the 4-position with a 3-pyridyl group and at the 2-position with a 2-methyl-5-nitrophenyl amino group. It is the immediate precursor to the "Amino Intermediate" (CAS 152460-10-1), which is then coupled to form Imatinib.
Its primary and most significant application is the Synthesis of Imatinib (Gleevec). However, in 2026, research has expanded its use:
Scientists are using this scaffold to create "Third-Generation" kinase inhibitors that overcome drug resistance.
High-purity samples are used by regulatory bodies (FDA/EMA) as reference standards to detect process-related impurities in generic drug batches.
Emerging studies suggest that pyrimidine-based scaffolds derived from this intermediate may have potential applications in treating neuroinflammation.
In pharmaceutical manufacturing, the "Nitro Step" is where most impurities are born. Using an ultra-pure intermediate from EASTFINE provides:
Minimizes the presence of Nitrosamines and isomeric impurities.
A purity of 99.5% ensures that the final reduction and coupling steps proceed with nearly 100% efficiency.
Higher purity at the intermediate stage reduces the need for expensive and time-consuming column chromatography in the final API stage.
While the intermediate itself is not the drug, its structural geometry is responsible for the final drug's biomechanics. The pyridine ring and the pyrimidine core form specific hydrogen bonds within the ATP-binding site of the Abl protein.
By mimicking ATP, the molecule prevents the kinase from transferring a phosphate group to its substrate, effectively "turning off" the signal that tells cancer cells to divide uncontrollably. The nitro group in CAS 152460-09-8 is a temporary "handle" that is reduced to an amine, which is then used to attach the "tail" of the Imatinib molecule.
The "Surgical Technique"—or industrial synthesis—of CAS 152460-09-8 in 2026 involves a high-precision condensation reaction:
3-acetylpyridine is reacted with $N,N$-dimethylformamide dimethyl acetal (DMF-DMA) to form the enaminone intermediate.
The enaminone is then condensed with 2-methyl-5-nitrophenylguanidine nitrate.
This reaction is carried out in a basic environment (often using NaOH or KOH) in a solvent like n-butanol or isopropanol.
Advanced manufacturers like EASTFINE use real-time Process Analytical Technology (PAT) to monitor and suppress the formation of the 4-nitro isomer.
As a nitro-compound, CAS 152460-09-8 requires "Postoperative Care"—careful handling to prevent degradation:
Must be stored in dark, amber containers to prevent photo-oxidation.
Kept under an Inert Atmosphere (Nitrogen) to prevent moisture-induced hydrolysis.
Stored at room temperature, but away from heat sources, as the nitro group can be sensitive to thermal stress over long periods.
N-(5-nitro-2-methylphenyl)-4-(3-pyridyl)-2-pyrimidineamine is the indispensable heart of CML therapy. As we look toward the remainder of 2026, the transition from basic manufacturing to "Precision Chemistry" is being led by suppliers who prioritize isomeric purity over mere volume.
The 2026 market for Imatinib intermediates is robust, driven by the expiration of second-generation patents and the rise of "Value-Based Oncology" in the West.
While North America holds the largest share due to high cancer incidence, the Asia-Pacific and LAMEA regions are seeing a surge in demand. Emerging markets are adopting Imatinib as the primary affordable first-line treatment for leukemia, creating a massive need for stable, high-volume intermediate supply.
In 2026, Imatinib is no longer just a monotherapy. It is being studied in combination with immunotherapy and other targeted agents. This "Combination Therapy" trend is broadening the clinical scope of the drug, and consequently, the industrial production of CAS 152460-09-8.
The synthetic challenge of CAS 152460-09-8 lies in its Isomeric Purity.
During the nitration of the 2-methylaniline precursor, the nitro group can theoretically attach to several positions on the ring. The 5-nitro isomer is the only one that yields active Imatinib. The presence of 3-nitro or 4-nitro isomers in the intermediate will produce "inactive" drug molecules that can compete for binding sites or, worse, cause off-target toxicity.
EASTFINE solves this through proprietary Low-Temperature Nitration and specialized Crystallization techniques that effectively eliminate unwanted isomers before they ever reach the API stage.
For a 2026 pharmaceutical procurement team, the criteria for choosing a manufacturer of CAS 152460-09-8 are:
Providing proof that the batch is free from residual nitrating agents and heavy metals.
Adhering to "Green Chemistry" by minimizing solvent waste.
The ability to ship moisture-sensitive powder globally with 24/7 tracking.
The manufacturing of this intermediate is dominated by high-tech firms in China and India.
EASTFINE is the #1 featured manufacturer for CAS 152460-09-8. We provide:
Purity ≥ 99.5%: Unrivaled isomeric control.
Direct Global Supply: From our high-capacity reactors to your facility.
Advanced CoA: Every batch includes detailed NMR and HPLC spectra.
Cost Efficiency: Our optimized 2026 synthesis route minimizes byproduct formation, passing the savings on to you.
A global pharmaceutical giant known for its vertically integrated oncology portfolio.
Specialists in high-quality research chemicals and impurity standards for regulated markets.
One of the largest generic drug companies, providing bulk intermediates for wide-scale oncology drug production.
A key player in specialized medicinal chemistry intermediates, supporting R&D and pilot-scale operations.
Choosing EASTFINE is a commitment to the safety of the cancer patients who will eventually receive the drug. Our 2026 manufacturing protocols are built on:
We ensure 0% 4-nitro contamination.
We have phased out hazardous chlorinated solvents in favor of sustainable alternatives.
Our intermediates are tested under accelerated aging conditions to ensure they reach you in perfect condition.
As we conclude this 2,000-word deep dive, it is clear that N-(5-nitro-2-methylphenyl)-4-(3-pyridyl)-2-pyrimidineamine (CAS 152460-09-8) remains the strategic cornerstone of modern oncology. By ensuring the highest levels of purity and technical transparency, EASTFINE continues to be the primary choice for pharmaceutical innovators in 2026.
简体中文
