The Trifunctional Pyridine Building Block for Pharmaceutical, Agrochemical, and Fine Chemical Synthesis: 2-Chloro-5-Formyl-4-Picoline (CAS# 884495-38-9)

2-Chloro-5-Formyl-4-Picoline (CAS# 884495-38-9), also known as 6-chloro-4-methylnicotinaldehyde, 6-chloro-4-methylpyridine-3-carboxaldehyde, or 6-chloro-4-methyl-3-pyridinecarboxaldehyde, is a polysubstituted pyridine derivative with the molecular formula C₇H₆ClNO and a molecular weight of 155.58 g/mol. Its molecular structure features a pyridine ring bearing three distinct functional groups: a chlorine atom at the 2-position (relative to the ring nitrogen), a formyl group (-CHO) at the 5-position, and a methyl group at the 4-position. This unique trifunctional substitution pattern—combining an electrophilic aldehyde, a nucleophilic chloro substituent, and a methyl group that provides steric and electronic modulation—confers exceptional versatility as a synthetic building block in medicinal chemistry, agrochemical development, and fine chemical synthesis. The compound typically appears as a colorless to pale yellow liquid with a boiling point of 277.6°C at 760 mmHg, a density of 1.269 g/cm³, a LogP of 1.86, and a topological polar surface area of 30 Ų. It is soluble in many organic solvents, including ethanol, ether, and chloroform, and is stable at room temperature, though it may decompose under heat, fire, or strongly acidic conditions. The compound is classified as a pharmaceutical intermediate and heterocyclic compound intermediate and is typically supplied at ≥95% to ≥98% purity.

Based on its chemical characteristics and industrial significance, this article systematically analyzes the key properties, core application areas, global market structure, regional dynamics, regulatory landscape, and future outlook of this strategically important trifunctional pyridine building block.

Core Application Fields and Demand

Market demand for 2-Chloro-5-Formyl-4-Picoline (CAS# 884495-38-9) is concentrated in three primary sectors: pharmaceutical synthesis and drug discovery (approximately 45–50% of global consumption), agrochemical development (approximately 25–30%), and fine chemical synthesis and research (approximately 20–25%). Its trifunctional nature and orthogonal reactivity serve as the core drivers of sustained demand growth across all sectors.

In pharmaceutical synthesis and drug discovery, 2-Chloro-5-Formyl-4-Picoline is an important intermediate in organic synthesis, frequently used in the preparation of other organic compounds. The compound serves as a valuable building block for the synthesis of pharmaceuticals, particularly in the preparation of substituted nitrogen-containing compounds, as evidenced by its appearance in patent literature for substituted nitrogen-containing compounds and imidazopyridine-pyrimidine derivatives. The formyl group provides a versatile handle for reductive amination, condensation, and Wittig reactions, while the chloro substituent enables nucleophilic aromatic substitution and cross-coupling reactions. The methyl group at the 4-position offers additional opportunities for functionalization and steric modulation of molecular properties.

In agrochemical development, 2-Chloro-5-Formyl-4-Picoline is used in the synthesis of agrochemicals. Its unique structural features—particularly the combination of electron-withdrawing chloro and formyl groups with an electron-donating methyl substituent—make it a versatile platform for constructing biologically active molecules targeting agricultural applications.

In fine chemical synthesis and research, 2-Chloro-5-Formyl-4-Picoline serves as a useful research chemical and building block for the preparation of other organic compounds. The compound’s ability to undergo multiple orthogonal transformations without the need for protecting group chemistry makes it particularly valuable for constructing complex molecular architectures efficiently. It is also used in the synthesis of other fine chemicals due to its unique structural features. The compound is classified as a heterocyclic compound intermediate and pyridine compound/methylpyridine intermediate.

In organic synthesis, 2-Chloro-5-Formyl-4-Picoline enables a wide range of transformations. The formyl group can be oxidized to carboxylic acids, reduced to alcohols, or converted to imines, oximes, and other derivatives. The chloro substituent can be displaced by various nucleophiles or participate in palladium-catalyzed cross-coupling reactions. The methyl group provides steric hindrance that can influence reaction selectivity and molecular conformation.

Key Properties and Reactivity Profile

2-Chloro-5-Formyl-4-Picoline (CAS# 884495-38-9) is a polysubstituted pyridine whose value derives from the orthogonal reactivity of its three functional groups.

Key physicochemical parameters include:

• Molecular Formula: C₇H₆ClNO
• Molecular Weight: 155.58 g/mol
• CAS Number: 884495-38-9
• EC Number: 810-633-1
• Synonyms: 6-Chloro-4-methylnicotinaldehyde; 6-chloro-4-methylpyridine-3-carboxaldehyde; 6-Chloro-4-methyl-3-pyridinecarboxaldehyde
• SMILES: CC1=CC(=NC=C1C=O)Cl
• InChIKey: GDOVQVRMRKHPNI-UHFFFAOYSA-N
• Appearance: Colorless to pale yellow liquid
• Boiling Point: 277.6°C at 760 mmHg
• Density: 1.269 g/cm³
• LogP: 1.86
• Topological Polar Surface Area: 30 Ų
• Hydrogen Bond Acceptors: 2
• Rotatable Bonds: 1
• Solubility: Soluble in ethanol, ether, chloroform, and many organic solvents
• Stability: Stable at room temperature; may decompose under heat, fire, or strongly acidic conditions
• Purity: ≥95% to ≥98% typical

The compound’s reactivity is defined by its three orthogonal handles: the formyl group (aldehyde) enables condensation, reductive amination, oxidation, and reduction reactions; the chloro substituent enables nucleophilic aromatic substitution (SNAr) and palladium-catalyzed cross-coupling; and the methyl group provides steric and electronic modulation while offering opportunities for further functionalization through radical or oxidation chemistry.

Major Market Participants

The global supply system for 2-Chloro-5-Formyl-4-Picoline (CAS# 884495-38-9) features a pattern of “specialized research chemical suppliers, multinational chemical distributors, and Chinese manufacturers serving distinct market segments.” As a specialized heterocyclic building block rather than a bulk commodity, the market is characterized by a moderate number of suppliers catering to pharmaceutical R&D, agrochemical development, and fine chemical synthesis.

In the global research and high-purity segment, key international suppliers include BOC Sciences, offering the compound as a useful research chemical; Fluorochem, supplying the compound from UK and Europe warehouses; AK Scientific (AKSci), offering 95% purity; TargetMol, supplying research-grade material; Apollo Scientific, offering the compound with GHS hazard warnings; and Aladdin Scientific, offering high-purity material at 96% purity. Other suppliers include BenchChem, CymitQuimica, and GlpBio. These suppliers serve the pharmaceutical, biotechnology, and academic research communities with products that meet rigorous quality specifications, typically at 95–98% purity. Packaging sizes range from 250 mg to 5 g and above.

In the industrial and large-scale production segment, Chinese manufacturers have emerged as a dominant force in the global supply chain. XinChem is a reliable manufacturer and supplier of high-purity 2-Chloro-5-Formyl-4-Picoline from China, offering the compound with stringent quality standards for use in pharmaceutical synthesis, agrochemical development, and fine chemical applications. Chinese suppliers offer the compound at various purity grades (typically 95–98%) and packaging options—from grams to bulk quantities—serving both domestic and export markets with competitive pricing.

Regional Market Dynamics

The global 2-Chloro-5-Formyl-4-Picoline market exhibits distinct regional characteristics, with production concentrated in Asia-Pacific (particularly China) and consumption distributed across North America, Europe, and the Asia-Pacific region, aligned with the pharmaceutical, agrochemical, and fine chemical industries in these regions.

The Asia-Pacific region has emerged as a significant production hub for 2-Chloro-5-Formyl-4-Picoline, with China hosting numerous manufacturers and suppliers including XinChem. The region’s competitive advantages include lower production costs, established chemical infrastructure, and proximity to rapidly growing pharmaceutical and agrochemical industries. Chinese suppliers offer the compound at various purity grades (typically 95–98%) and packaging options, serving both domestic and export markets. The growing pharmaceutical R&D, agrochemical, and fine chemical sectors in China, India, Japan, and South Korea continue to drive regional consumption growth.

North America remains a key market for high-purity and research-grade 2-Chloro-5-Formyl-4-Picoline, driven by demand from the pharmaceutical industry, biotechnology companies, and academic research institutions. The United States hosts numerous research organizations, pharmaceutical companies, and contract research organizations that require high-quality heterocyclic building blocks for drug discovery and development. Suppliers such as BOC Sciences and AK Scientific serve the North American market. The region’s well-established regulatory framework and emphasis on product quality support demand for high-grade research chemicals and pharmaceutical intermediates.

Europe is characterized by stringent regulatory requirements and a strong focus on quality and sustainability in pharmaceutical and chemical research. European pharmaceutical companies, agrochemical developers, and research institutions demand high-purity heterocyclic building blocks with comprehensive documentation. Suppliers such as Fluorochem (UK) and Apollo Scientific serve the European market with in-stock availability.

Japan represents a specialized market where 2-Chloro-5-Formyl-4-Picoline is supplied by distributors for pharmaceutical research, agrochemical development, and fine chemical applications.

Regulatory and Safety Considerations

As a research chemical, pharmaceutical intermediate, and agrochemical building block, 2-Chloro-5-Formyl-4-Picoline (CAS# 884495-38-9) is subject to regulatory oversight in major global economies. Compliance with relevant regulations is essential for market access and trade.

GHS classification and handling: 2-Chloro-5-Formyl-4-Picoline is classified with the signal word “Warning”. Hazard statements include H302 (Harmful if swallowed), H315 (Causes skin irritation), H319 (Causes serious eye irritation), H335 (May cause respiratory irritation), and H302+H312+H332 (Harmful if swallowed, in contact with skin or if inhaled). The compound is classified as Acute Toxicity – Oral Category 4 and Eye Irritation Category 2. Precautionary statements include P264 (Wash skin thoroughly after handling), P270 (Do not eat, drink or smoke when using this product), P280 (Wear protective gloves/protective clothing/eye protection/face protection), P301+P312 (IF SWALLOWED: Call a POISON CENTER/doctor if you feel unwell), P305+P351+P338 (IF IN EYES: Rinse cautiously with water for several minutes; remove contact lenses if present and easy to do; continue rinsing), P330, P337+P313, and P501. The compound is classified as harmful (Xn) with risk codes R22 (Harmful if swallowed) and R36 (Irritating to eyes). Safety description 26 advises: “In case of contact with eyes, rinse immediately with plenty of water and seek medical advice”.

Storage and handling: The compound should be stored in a cool, dry and well-ventilated area, away from fire and oxidants. Avoid inhalation, skin contact, and ingestion during handling and use. Appropriate personal protective equipment (such as gloves, safety glasses, and protective clothing) should be worn when handling the compound. In case of contact, rinse contaminated skin with plenty of water and seek medical attention.

Transport information: 2-Chloro-5-Formyl-4-Picoline is not classified as hazardous material for DOT/IATA transport purposes. Proper packaging, labeling, and documentation are nevertheless required for international shipping in compliance with the International Maritime Dangerous Goods Code (IMDG Code) and other transport regulations. The compound is classified as a combustible liquid.

Regulatory compliance: In the European Union, the compound must comply with REACH registration requirements and CLP classification under Regulation (EC) No 1272/2008 for import and use. Manufacturers and suppliers must provide comprehensive Safety Data Sheets (SDS) and maintain appropriate documentation. In the United States, 2-Chloro-5-Formyl-4-Picoline is intended for research and development use only and is not intended for therapeutic, food, cosmetic, or consumer applications unless explicitly stated otherwise. For pharmaceutical intermediate applications, manufacturers must comply with relevant FDA regulations and quality standards.

Future Outlook

The market outlook for 2-Chloro-5-Formyl-4-Picoline is positive, supported by several key growth drivers across its major application segments. While the compound remains a relatively specialized heterocyclic building block, its trifunctional nature and orthogonal reactivity position it for steady growth in the coming years.

Key growth drivers include:

1. Expansion of pharmaceutical R&D and drug discovery: Increasing investment in drug discovery and development, particularly in heterocyclic medicinal chemistry, supports demand for versatile pyridine building blocks with orthogonal functional groups.
2. Growth in agrochemical development: The growing global demand for novel agrochemicals—driven by increasing food production needs and the development of more selective crop protection agents—supports consumption of the compound as a precursor for biologically active molecules.
3. Increasing demand for fine chemicals: The expanding market for fine chemicals, including pharmaceuticals, agrochemicals, and specialty materials, drives demand for high-purity heterocyclic intermediates.
4. Advantages of trifunctional building blocks: The compound’s ability to undergo selective, sequential functionalization without protecting group chemistry makes it increasingly valuable in modern synthetic chemistry, particularly for constructing complex molecular architectures efficiently.
5. Growth in contract research and manufacturing organizations (CROs/CDMOs): Increasing outsourcing of pharmaceutical R&D and manufacturing to CROs and CDMOs drives demand for high-quality building blocks and intermediates.

Challenges and considerations:

• Regulatory compliance: Increasingly stringent pharmaceutical, agrochemical, and chemical regulations may require ongoing investment in quality systems and documentation.
• Competition from alternative building blocks: The market faces competition from other substituted pyridines and heterocyclic building blocks with similar reactivity profiles.
• Limited scale: As a relatively specialized compound, the market for 2-Chloro-5-Formyl-4-Picoline is smaller than that of commodity chemicals.
• Handling requirements: The compound’s classification as harmful (H302, H315, H319, H335) requires appropriate safety measures during handling and storage.

To succeed in this evolving market landscape, suppliers must focus on product quality (particularly purity and batch-to-batch consistency), supply chain reliability, regulatory compliance, and responsive customer service. Companies that can offer high-purity products, flexible packaging options, and technical support for pharmaceutical, agrochemical, and fine chemical applications will be well-positioned to capture growing demand.

Shanghai XinChem Co., Ltd. (XinChem)

As a world-leading supplier of organic chemicals and heterocyclic building blocks, Shanghai XinChem Co., Ltd. (XinChem) is dedicated to meeting the innovative needs of the pharmaceutical, agrochemical, fine chemical, and research industries. Leveraging extensive experience and advanced manufacturing capabilities, XinChem provides high-quality 2-Chloro-5-Formyl-4-Picoline (CAS# 884495-38-9) to customers worldwide. As a trusted manufacturer and supplier based in China, XinChem combines competitive pricing, reliable supply, and exceptional service to establish itself as a preferred partner for research institutions, pharmaceutical companies, and industrial manufacturers seeking this versatile trifunctional pyridine building block.

1. Technical Advantages

Advanced Synthesis and Purification Processes
XinChem utilizes state-of-the-art manufacturing facilities and rigorous quality control measures to ensure the purity, consistency, and safety of its 2-Chloro-5-Formyl-4-Picoline products. The production process incorporates established synthetic routes—including the treatment of 4-methylpyridine with alkali to generate the corresponding negative ions, followed by reaction with cuprous chloride to form alkyl copper intermediates, which are then reacted with formaldehyde to yield 6-chloro-4-methylpyridine-3-carboxaldehyde—enabling the delivery of products with purity ≥95% to ≥98% to meet diverse application requirements. Strict process control ensures consistent product quality, minimal impurities, and batch-to-batch reproducibility, providing customers with reliable performance in pharmaceutical synthesis, agrochemical development, and fine chemical applications.

Full-Chain Quality Control
The production process strictly adheres to international quality standards, with comprehensive quality control covering raw material sourcing, in-process monitoring, and finished product testing. Each batch is accompanied by a detailed Certificate of Analysis (COA) documenting physical and chemical properties, purity data (HPLC/GC), and impurity profiles. This commitment to quality ensures that XinChem’s 2-Chloro-5-Formyl-4-Picoline meets the stringent requirements of pharmaceutical R&D, agrochemical development, and research applications.

2. Product Advantages

High Purity and Consistent Quality
XinChem offers 2-Chloro-5-Formyl-4-Picoline with purity ≥95% to ≥98% (HPLC/GC), ensuring optimal performance in pharmaceutical synthesis, agrochemical development, and fine chemical applications. The product’s high purity minimizes the risk of unwanted side reactions and impurities, making it suitable for demanding applications in drug discovery, crop protection, and specialty chemical synthesis.

Comprehensive Specifications
Key specifications include:

• Molecular Formula: C₇H₆ClNO
• Molecular Weight: 155.58 g/mol
• CAS Number: 884495-38-9
• Synonyms: 6-Chloro-4-methylnicotinaldehyde; 6-chloro-4-methylpyridine-3-carboxaldehyde; 6-Chloro-4-methyl-3-pyridinecarboxaldehyde
• MDL Number: MFCD03452747
• Appearance: Colorless to pale yellow liquid
• Purity: ≥95% to ≥98% (HPLC/GC)
• Boiling Point: 277.6°C at 760 mmHg
• Storage: Cool, dry, well-ventilated area, away from fire and oxidants

Flexible Packaging Solutions
XinChem provides a range of packaging options to accommodate diverse customer needs, from laboratory-scale quantities (grams) to industrial-scale packaging (kilograms) and bulk shipments. Customized packaging solutions are available upon request, ensuring safe handling, storage, and transportation.

3. Application Fields

As a versatile trifunctional pyridine building block, 2-Chloro-5-Formyl-4-Picoline (CAS# 884495-38-9) exhibits wide application value across multiple industries:

Pharmaceutical Synthesis and Drug Discovery:

• Important intermediate in organic synthesis for pharmaceutical preparation
• Building block for substituted nitrogen-containing compounds
• Precursor for imidazopyridine-pyrimidine derivatives
• Versatile platform for constructing complex drug-like molecules

Agrochemical Development:

• Building block for agrochemical synthesis
• Precursor for biologically active molecules for crop protection

Fine Chemical Synthesis:

• Useful research chemical for organic synthesis
• Building block for the preparation of other organic compounds
• Heterocyclic compound intermediate

Organic Synthesis and Research:

• Trifunctional building block enabling selective, orthogonal transformations
• Reagent for medicinal chemistry and chemical biology research

4. Service Support

Technical Expertise and Customized Solutions
XinChem’s team of experienced chemists and application engineers provides full technical support throughout the customer journey—from product selection and specification development to application guidance and troubleshooting. Whether customers require optimization of synthetic routes, guidance on orthogonal functionalization strategies, or assistance with regulatory documentation, XinChem’s technical experts are ready to help. Custom synthesis and contract manufacturing with flexible scaling from R&D to commercial quantities are available upon request.

Global Logistics and Reliable Supply
With established supply chains serving markets across Europe, North America, Asia-Pacific, and beyond, XinChem ensures timely delivery and consistent product availability. The company’s logistics team manages all aspects of international shipping, including customs clearance and documentation, with appropriate handling for research chemicals and intermediates.

Regulatory Support
XinChem provides comprehensive documentation to support regulatory compliance, including Safety Data Sheets (SDS), Certificates of Analysis (COA), and other required certificates. The company stays current with evolving regulatory requirements in major markets, including REACH, TSCA, and other regional regulations, helping customers navigate the complexities of global trade.

5. Reasons to Choose XinChem

• Professionalism: Extensive experience and deep expertise in heterocyclic building block synthesis and supply.
• Quality: Rigorous quality control, high purity (≥95% to ≥98%), and adherence to international standards.
• Reliability: Stable supply, competitive pricing, and timely delivery.
• Flexibility: Customized solutions to meet diverse customer needs, including custom synthesis and packaging.
• Service: Responsive technical support and comprehensive documentation.

Contact us today to start your partnership with XinChem!

Website: www.xinchem.com

Email: sales1@xinchem.com

WhatsApp: +86 18049800532