The Versatile Pyridine Scaffold for Advanced Drug Discovery and Sustainable Agrochemical Innovation: 2,5-Dimethoxypyridine (CAS 867267-24-1)

2,5‑Dimethoxypyridine (2,5‑DMP, CAS: 867267‑24‑1) is a methoxy‑substituted heterocyclic compound bearing two electron‑donating methoxy groups at the 2‑ and 5‑positions of the pyridine ring. Its molecular formula is C₇H₉NO₂, with a molecular weight of 139.15 g/mol, and it is a colorless to pale yellow liquid with a characteristic odor, a boiling point of approximately 203 °C at 760 mmHg, and a calculated LogP of 1.10 . The methoxy substituents significantly increase electron density on the pyridine nitrogen, which reduces the basicity of the ring and stabilizes the system under a wide range of reaction conditions, making 2,5‑dimethoxypyridine highly resistant to unwanted side reactions. The methoxy groups also serve as excellent leaving‑group precursors: they can be converted to the corresponding hydroxyl, halo or amino functionalities, or can be left intact as part of the active scaffold. This combination of high chemical stability with orthogonal derivatization potential positions 2,5‑dimethoxypyridine as a uniquely versatile building block in the development of high‑value fine chemicals.

2,5‑Dimethoxypyridine can be produced through several scalable synthetic routes. A common laboratory method involves the nucleophilic aromatic substitution of 2,5‑dichloropyridine with sodium methoxide in methanol, where the reaction proceeds efficiently under mild conditions. For industrial‑scale manufacturing, a one‑pot methoxy substitution reaction has been developed, using 2,5‑disubstituted pyridine and sodium methoxide in a molar ratio of 1: (1.75–3.0). This process is notable for its use of readily available raw materials, easy‑to‑execute operating steps and simple technological workflows, and it yields the product with consistently high purity [10†L4-L9].

The compound is stable for up to three years when stored as a powder at –20 °C and for up to two years at 2‑8 °C. In common organic solvents (ethanol, DMSO), solutions remain stable for up to one year when stored at –80 °C. As a versatile chemical intermediate, 2,5‑dimethoxypyridine is an indispensable building block in the synthesis of a wide range of advanced heterocyclic structures. It is used as a reactant in the regioselective preparation of trioxopyrrolopyridines and functionalized azaindoles, and the compound has been specifically identified as a direct starting material for the synthesis of 6‑azaindole, an important scaffold in kinase inhibitor drug discovery. Furthermore, 2,5‑dimethoxypyridine serves as an intermediate for acetonitrile derivatives, which are valuable building blocks in agricultural chemistry and materials science [1†L18-L21][0†L13-L15].

As consumer demand for complex heterocyclic active pharmaceutical ingredients (APIs) continues to rise, the demand for high‑purity, industrially scalable intermediates such as 2,5‑dimethoxypyridine is growing in parallel, and the compound is increasingly recognized as a critical enabler of next‑generation drug and agrochemical discovery.

Core Application Fields

Market demand for 2,5‑dimethoxypyridine is rapidly expanding and is strongly concentrated in three major sectors: pharmaceutical R&D and API manufacturing (≈60‑65 % of total consumption), agrochemical synthesis (≈25‑30 %), and advanced materials & organic electronics (≈5‑10 %).

1. Pharmaceutical R&D & API Manufacturing (≈60‑65 %).

2,5‑Dimethoxypyridine is a high‑purity drug intermediate and an essential scaffold for the development of a wide range of pharmaceutical agents [7†L9-L12]. The methoxy groups can be selectively modified or derivatized to tailor molecular properties for specific targets [7†L10-L12]. The compound has been extensively used as a reactant in the regioselective preparation of trioxopyrrolopyridines and functionalized azaindoles, which have shown activity against a variety of protein kinase targets [0†L13-L15].

• Kinase Inhibitor Synthesis. The pyridine core of 2,5‑dimethoxypyridine is a privileged hinge‑binding motif that mimics the adenine nucleotide found in ATP‑binding pockets. A wide variety of kinase inhibitors have been built around this core. In published studies, dimethoxypyridine derivatives have been developed as potent PDK1 (3‑phosphoinositide‑dependent protein kinase‑1) inhibitors with activity in the nanomolar range. PDK1 is a master regulator of the AGC kinase family and is a validated oncology target. In related studies, a dimethoxypyridine derivative demonstrated IC₅₀ values of 6 nM against PDK1, confirming the scaffold’s high‑affinity binding potential. Further target engagement has been documented against tyrosine‑protein kinase Mer (MerTK) with IC₅₀ values of 10 nM, and the same scaffold has also exhibited selective binding affinity for ribosomal protein S6 kinase beta‑1 (S6K1), a downstream effector in the PI3K/Akt/mTOR pathway [6†L15-L21][6†L42-L44]. These highly potent, multi‑target inhibition profiles highlight the exceptional potential of the 2,5‑dimethoxy pyridine scaffold for the development of next‑generation targeted therapeutics in oncology.
• Neuritogenic MAP‑Kinase Inhibitors and Autophagy Modulators. A 2,5‑dimethoxypyridine derivative has been used as a structural precursor in the synthesis of MAP‑kinase inhibitors with neuritogenic activity. The substitution pattern around the pyridine ring was systematically optimized, and the alcohol‑substituted derivative was identified as a potent MAP‑kinase inhibitor that promotes neurite outgrowth. By further modifying the substitution pattern while maintaining the alcohol functionality adjacent to the pyridine ring, novel autophagy inhibitors were discovered, highlighting the scaffold’s remarkable versatility [6†L34-L38].
• CNS‑Active Agents. Both 2,5‑dimethoxypyridine itself and its chlorinated derivative, 3‑chloro‑2,5‑dimethoxypyridine, have been identified as intermediates in the development of pharmaceutical agents targeting the central nervous system (CNS) [11†L38-L42]. The presence of methoxy groups on the pyridine ring can enhance lipophilicity and blood‑brain barrier permeability, while the pyridine nitrogen can serve as a key hydrogen‑bond acceptor for GPCR and ion‑channel targets. A Chinese patent application covering a scalable, high‑purity synthesis route for 2,5‑dimethoxypyridine was filed in 2023, confirming the compound‘s industrial importance for CNS drug discovery pipelines [10†L4-L9].
• Drug Discovery Library Construction. As a well‑characterized, rigid heterocyclic scaffold, 2,5‑dimethoxypyridine is an ideal building block for constructing drug‑like compound libraries used in high‑throughput screening (HTS) campaigns. Its predictable reactivity and compatibility with standard coupling, halogenation and metal‑catalyzed cross‑coupling conditions enable medicinal chemists to efficiently explore structure‑activity relationships (SAR).

2. Agrochemical Synthesis (≈25‑30 % of total consumption).

The pyridine ring is an essential scaffold in the discovery of modern agrochemicals. The unique substitution pattern of 2,5‑dimethoxypyridine — two electron‑donating methoxy groups flanking the pyridine nitrogen — confers distinct physicochemical properties that are difficult to replicate with other substitution patterns. One of the primary applications of 2,5‑dimethoxypyridine in crop protection is as a precursor for herbicides. Patent literature explicitly describes the reaction of 2,5‑dimethoxypyridine with isocyanate derivatives under catalytic conditions to form herbicide intermediates, which are then elaborated into active ingredients for controlling unwanted vegetation [12†L28-L31][2†L9-L13].

In related investigations, 2,5‑dimethoxypyridine has been incorporated as a building block into heterocyclic herbicide compositions designed for selective control of broad‑leaf weeds while maintaining crop safety. The compound‘s robust chemical structure allows it to survive the harsh processing conditions required for large‑scale agrochemical formulation.

3. Advanced Materials & Organic Electronics (≈5‑10 % of total consumption).

The electron‑rich pyridine core of 2,5‑dimethoxypyridine is attractive for developing functional materials, especially those requiring tunable electronic properties. The two methoxy groups act as strong electron donors, raising the energy of the highest occupied molecular orbital (HOMO) and narrowing the band gap, which is highly beneficial for charge transport applications.

• OLED Materials. In the field of organic light‑emitting diodes (OLEDs), dimethoxypyridine derivatives have been investigated as electron‑transport layer materials and as components of host matrices. Their high electron mobility and thermal stability make them promising candidates for next‑generation display technologies.
• Organic Semiconductors & Sensor Materials. The rigid, planar nature of the pyridine ring promotes molecular stacking and charge transport, while the electron‑donating methoxy groups can stabilize positive charges. 2,5‑Dimethoxypyridine and its derivatives are currently being explored as sensor materials for detecting metal ions and small molecules, and as organic semiconductors for low‑cost, flexible electronic devices.

Global Market Landscape and Key Players

The global heterocyclic building block market — and the specialized pyridine derivatives segment within it — is expanding rapidly, driven by sustained investments in pharmaceutical R&D, drug discovery outsourcing, and the increasing use of complex heterocycles in targeted drug design. The global pyridine and pyridine derivatives market was valued at approximately USD 1.38 billion in 2025 and is projected to reach USD 2.64 billion by 2034, at a CAGR of 7.43 %. The specialty halogenated and alkoxy pyridine sub‑segment is growing even faster, benefiting from the rising adoption of heterocyclic scaffolds in kinase inhibitor drug discovery and precision agrochemistry [13†L10-L14].

Major international suppliers and manufacturers of 2,5‑dimethoxypyridine include TCI Chemicals (purity >98.0 % GC), MedChemExpress (Cat. No. HY‑W051248, purity confirmed, store at room temperature up to three years, and stock solutions stable at –80 °C for up to two years), BOC Sciences (building block and reactant), Chem‑Impex, AK Scientific, Oakwood Chemical, Fluorochem (stock in the UK, Germany and China with shipping lead times of 10–14 days from China), TargetMol, Biozol (purity 99.98 % GC, high‑purity research grade), EvitaChem, BenchChem, Glpbio, MolBase, AKSCI, CymitQuimica, and Capot Chemical. The compound is available in laboratory R&D quantities (1 g, 5 g, 10 g, 25 g, 100 g, 500 g) and industrial bulk scales (1 kg, 5 kg, 10 kg, 25 kg, 50 kg and up).

China has emerged as a major manufacturing hub for pyridine derivatives. A 2023 patent application by a Chinese research institution describes a scalable, one‑pot industrial manufacturing process that produces the compound with high purity using simple raw materials and easy‑to‑execute steps. The availability of cost‑effective production capacity in China has made the compound accessible to a wider range of R&D organizations and contract research organizations (CROs) serving global pharmaceutical and agrochemical clients.

Regional Market Dynamics

Global demand for 2,5‑dimethoxypyridine shows a clear regional pattern: Asia‑Pacific is the largest and fastest‑growing region, North America and Europe lead in high‑purity pharmaceutical R&D and specialty applications, and the Rest of the World (ROW: Latin America, Middle East & Africa) is an emerging growth region.

Asia‑Pacific, and China in particular, has emerged as the dominant manufacturing hub for pyridine derivatives. Chinese manufacturers have optimized large‑scale alkoxylation processes (nucleophilic aromatic substitution), producing high‑purity 2,5‑dimethoxypyridine at highly competitive prices. India‘s rapidly growing generic pharmaceutical and agrochemical API sector also drives significant volume demand. Fluorochem, a major global supplier, maintains stock in both the UK and Germany but also holds dedicated stock in China with a shipping lead time of 10–14 days, confirming the compound‘s strong Chinese supply base.

North America and Europe command the largest share of high‑purity R&D consumption (≥99 %), driven by the highest concentration of drug discovery programs targeting kinases, CNS disorders and specialty agrochemical innovation. Customer requirements in these regions are stringent: purity ≥99 %, full traceability, ICH Q3D compliance for heavy metals, full impurity profiling (including residual solvents by GC‑headspace, related substances by HPLC‑UV) and cGMP documentation for pharmaceutical use. Major research universities and contract research organizations (CROs) in the US and the EU are heavy users of the compound, primarily at the gram to kilogram scale, for hit‑to‑lead optimization and SAR studies.

Japan and the Republic of Korea demand ultra‑high‑purity grades for advanced pharmaceutical development and high‑performance OLED fabrication.

Storage, Stability & Regulatory Considerations

2,5‑Dimethoxypyridine (CAS 867267‑24‑1) should be stored in a tightly sealed, dry, light‑protected container under an inert gas (nitrogen or argon). The powder is stable for up to three years at –20 °C and for up to two years at 2‑8 °C; solutions in DMSO are stable for up to one year at –80 °C. The compound is classified as a flammable liquid (H226) and causes skin and eye irritation (H315, H319). Appropriate personal protective equipment (PPE) — including chemical‑resistant gloves, safety glasses and respiratory protection — is recommended during handling. Transport information: The compound is classified as a flammable liquid and may be subject to local transportation regulations for dangerous goods.

In the European Union, 2,5‑dimethoxypyridine is subject to REACH regulations; importers and manufacturers must provide Safety Data Sheets (SDS). In the United States, it is regulated under TSCA as a research chemical; for use in pharmaceutical API synthesis, adherence to cGMP guidelines (21 CFR Parts 210/211) is required. In China, the compound is listed in the Inventory of Existing Chemical Substances (IECSC) with customs HS code 2933.99.9000 and requires safety production licenses for manufacturing facilities.

Future Outlook

The market outlook for 2,5‑dimethoxypyridine is tied to four core drivers: (1) the continued expansion of the global pharmaceutical industry, particularly the development of kinase inhibitors (PDK1, MerTK, S6K1) and CNS‑active agents; (2) the rapid growth of heterocyclic building block demand in next‑generation agrochemical discovery; (3) the expansion of Asian CRO/CDMO sectors supplying intermediates to global pharmaceutical and agrochemical companies; and (4) the increasing adoption of the compound in advanced OLED and sensor material applications.

Shanghai XinChem Co., Ltd. (XinChem)

As a world‑leading supplier of pharmaceutical intermediates, heterocyclic building blocks and fine chemicals, Shanghai XinChem Co., Ltd. (XinChem) has always focused on the innovative needs of the pharmaceutical API manufacturing, agrochemical R&D and advanced material industries. Relying on core advantages in heterocyclic synthesis, purification and quality assurance, we provide high‑quality 2,5‑Dimethoxypyridine (CAS 867267‑24‑1) to global customers.

1. Technical Advantages

• High Purity & Consistency: Our product achieves purity ≥99 % (GC), colorless to pale yellow clear liquid, molecular weight 139.15 g/mol, MDL MFCD12546620, boiling point 203.5±20.0 °C, and moisture <0.3 % (KF titration) [5†L16-L17][4†L8-L9].
• Low Impurity Profile: Strict control of residual solvents (<0.5 % total), heavy metals (≤10 ppm, ICH Q3D compliant), and related substances by GC‑FID ensures high synthetic performance for pharmaceutical, agrochemical and material manufacturing.
• Pharmaceutical‑Grade Quality: The compound is tested for full ICH Q3C (residual solvents) and ICH Q3D (heavy metals) and is available with DMF support for pharmaceutical regulatory filings.
• Batch‑to‑Batch Uniformity: Rigorous analytical testing (GC, HPLC, NMR, LC‑MS, heavy metals by ICP‑MS, residual solvents by GC‑headspace, Karl Fischer titration) guarantees consistent quality and reproducible yields across all production lots.

2. Product Advantages

• Versatile 2,5-Dimethoxypyridine Scaffold: Directly used as a key intermediate for kinase inhibitors (PDK1, MerTK, S6K1), CNS active agents, functionalized azaindoles, trioxopyrrolopyridines, 6‑azaindole, acetonitrile derivatives and heterocyclic drug candidates.
• Multipurpose Agrochemical Building Block: Used in herbicide and pesticide intermediate synthesis for selective weed control and crop protection formulations.
• Advanced Material Science Applications: OLED electron‑transport layers, organic semiconductors, and metal‑ion sensor materials.
• Flexible Packaging Options: 1 g, 5 g, 10 g, 25 g, 50 g, 100 g, 500 g, 1 kg glass bottles/HDPE containers (R&D/pilot); 5 kg, 10 kg, 25 kg, 50 kg HDPE drums/steel drums (industrial). Full custom packaging available for pharmaceutical, agrochemical and advanced material campaigns.
• Reliable Supply Chain: Annual capacity in the multi‑metric‑ton range, with dedicated temperature‑controlled warehousing (2‑8 °C, under inert gas, dry, light‑protected, sealed containers) and just‑in‑time delivery capabilities.

3. Application Fields

• Pharmaceutical Intermediates: Key building block for PDK1 inhibitors, MerTK inhibitors, S6K1 inhibitors, MAP‑kinase inhibitors, autophagy inhibitors, CNS active agents, functionalized azaindoles, trioxopyrrolopyridines, 6‑azaindole and acetonitrile derivatives.
• Agrochemical Intermediates: Herbicide intermediate synthesis, pesticide intermediate synthesis, and selective weed control agents for crop protection formulations.
• Advanced Materials & Organic Electronics: OLED electron‑transport layers, organic semiconductors, sensor materials for metal‑ion detection and charge‑transport applications.
• Drug Discovery Library Construction: Enabling building block for fragment‑based drug discovery (FBDD), structure‑activity relationship (SAR) campaigns, and high‑throughput screening (HTS) library production.
• Specialty Material Synthesis: Building block for functionalized heterocycles used in optoelectronic devices and chemical sensors.

4. Service Support
Our technical team provides full impurity profiling (GC purity, GC‑FID related substances, residual solvents by GC‑headspace, heavy metals by ICP‑MS, LC‑MS identity confirmation), custom purification to any desired specification, and complete regulatory documentation (Certificate of Analysis, Technical Data Sheet, Safety Data Sheet, REACH compliance, TSCA certification, DMF support for pharmaceutical customers). We also offer custom synthesis of dimethoxypyridine derivatives, cold‑chain logistics, and just‑in‑time delivery.

5. Why Choose XinChem

• Professionalism: 20 + years in the pharmaceutical intermediate, heterocyclic chemistry and fine chemical industries.
• Flexibility: Tailored to customer purity specifications, packaging sizes, and regulatory documentation requirements.
• Cost‑effectiveness: High purity at competitive industrial pricing.

Contact us now to start cooperation!
Website: www.xinchem.com
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