The Fluorinated Benzophenone Building Block for Pitavastatin, Fluorescent Probes, and Pharmaceutical Intermediates: 2-Amino-4′-fluorobenzophenone (CAS# 3800-06-4)

2-Amino-4′-fluorobenzophenone (CAS# 3800-06-4), also known as (2-aminophenyl)(4-fluorophenyl)methanone or 2-amino-4′-fluorodiphenylmethanone, is a fluorinated benzophenone derivative with the molecular formula C₁₃H₁₀FNO and a molecular weight of 215.22 g/mol. Its molecular structure consists of a benzophenone core bearing a primary amino group at the 2-position of one phenyl ring and a fluorine atom at the 4′-position of the other ring. This specific substitution pattern—distinguishing it from other amino-fluorobenzophenone regioisomers—confers unique electronic and steric properties that directly influence its reactivity, hydrogen-bonding capability, and the biological activity of downstream derivatives.

As a light yellow to off-white crystalline powder with a melting point of 124–131°C and a density of 1.236 g/cm³, the compound exhibits good solubility in chloroform and DMSO (25 mg/mL), but low solubility in water. It is classified as an irritant (H315, H319, H335) and is air-sensitive, requiring storage under argon in a cool, dark place (recommended below 15°C) to prevent oxidative degradation. The compound is typically supplied at ≥98% purity (GC and non-aqueous titration).

2-Amino-4′-fluorobenzophenone is a strategically important fluorinated building block that serves as the key intermediate in the synthesis of Pitavastatin—a potent, third-generation HMG-CoA reductase inhibitor for the treatment of hypercholesterolemia and prevention of cardiovascular disease. Beyond its flagship pharmaceutical application, the compound functions as a precursor for p-fluorobenzoyl chloride and as a fluorescent probe for DNA and RNA detection in biochemical research. Its derivatives are employed as fluorescence derivatization reagents for aromatic aldehydes in liquid chromatography, and the compound serves as a building block for dyes, pesticides, and other pharmaceutical intermediates. Based on its chemical characteristics and industrial significance, this article systematically analyzes the key properties, core application areas, global market structure, regulatory landscape, and future outlook of this strategically important fluorinated aromatic building block.

Key Properties and Reactivity Profile

2-Amino-4′-fluorobenzophenone (CAS# 3800-06-4) is a regioisomer-specific fluorinated benzophenone whose value derives from the orthogonal reactivity of its amino, carbonyl, and fluorine functionalities.

Key physicochemical parameters include:

• Molecular Formula: C₁₃H₁₀FNO
• Molecular Weight: 215.22 g/mol
• CAS Number: 3800-06-4
• MDL Number: MFCD06658166
• Synonyms: (2-Aminophenyl)(4-fluorophenyl)methanone; 2-Amino-4′-fluorodiphenylmethanone
• Appearance: Light yellow to off-white crystalline powder
• Purity: ≥98.0% (GC) / ≥98.0% (non-aqueous titration)
• Melting Point: 124–131°C (literature 127–131°C; TCI specification 127.0–131.0°C)
• Density: 1.236 g/cm³ (predicted)
• Solubility: Chloroform (soluble); DMSO (25 mg/mL, 116.16 mM); low solubility in water
• Storage: Under argon, cool and dark place (recommended below 15°C); powder stable for 3 years at -20°C
• SMILES: Nc1ccccc1C(=O)c1ccc(F)cc1
• InChIKey: FYUBQQXQLLYNJG-UHFFFAOYSA-N
• GHS Classification: Warning; H315 (Causes skin irritation), H319 (Causes serious eye irritation), H335 (May cause respiratory irritation)
• HS Code: 2922.39-000 (Japan export)

The compound’s reactivity is defined by its three orthogonal handles: the amino group at C2 enables diazotization, acylation, and Schiff base formation; the ketone carbonyl provides a site for nucleophilic addition, reduction, and condensation reactions; and the fluorine atom at C4′ modulates the electronic environment of the ring and enhances metabolic stability of downstream derivatives. The 2-amino-4′-fluoro substitution pattern is critical for the compound’s utility—the amino group ortho to the carbonyl facilitates intramolecular hydrogen bonding and directs electrophilic substitution, while the fluorine atom para to the carbonyl modulates the electronic environment and improves the pharmacokinetic profile of Pitavastatin. Substituting one regioisomer for another (e.g., 2-amino-4-fluorobenzophenone or 2-amino-5-fluorobenzophenone) would result in significantly different reactivity, hydrogen-bonding capability, and biological activity.

Core Application Fields and Demand

Market demand for 2-amino-4′-fluorobenzophenone (CAS# 3800-06-4) is concentrated in three primary sectors: pharmaceutical synthesis and drug intermediates (approximately 55–60% of global consumption), fluorescent probes and biochemical research (approximately 20–25%), and dyes, pesticides, and specialty chemicals (approximately 20–25%). Its unique combination of an ortho-amino-carbonyl motif with a strategically positioned fluorine atom serves as the core driver of sustained demand growth.

In pharmaceutical synthesis and drug intermediates, 2-amino-4′-fluorobenzophenone is a pivotal intermediate in the synthesis of numerous active pharmaceutical ingredients (APIs), most notably as a precursor to Pitavastatin (Livalo®)—a potent, third-generation HMG-CoA reductase inhibitor used for the treatment of hypercholesterolemia and prevention of cardiovascular disease. Pitavastatin is characterized by its potent cholesterol-lowering efficacy, favorable safety profile, and minimal drug-drug interactions compared to earlier statins. The synthesis of Pitavastatin from 2-amino-4′-fluorobenzophenone typically involves a multi-step process, including cyclocondensation to form the quinoline core, followed by side-chain installation and resolution. The compound also serves as an important intermediate in the development of anti-cancer agents and other therapeutic drugs. Its derivatives have been investigated for anti-inflammatory activity, with studies demonstrating their potential as inhibitors of key cytokines and enzymes involved in the inflammatory process. The compound is also employed as a reference standard for API quality control and analytical method validation.

In fluorescent probes and biochemical research, 2-amino-4′-fluorobenzophenone and its derivatives are utilized as fluorescent probes for DNA and RNA detection in biochemical studies. The compound’s fluorescence properties, derived from the benzophenone scaffold, are modulated by the amino and fluorine substituents, enabling the development of probes with tailored optical properties. Its derivatives have been used as fluorescence derivatization reagents for aromatic aldehydes in liquid chromatography, improving detection sensitivity and specificity in analytical chemistry applications. These probes find applications in live-cell imaging, nucleic acid detection, and diagnostic assays.

In dyes, pesticides, and specialty chemicals, 2-amino-4′-fluorobenzophenone is used as an intermediate for dyes and pesticides, as well as in organic synthesis and material science. The compound serves as a Friedel-Crafts acylation reagent and can be used to synthesize quinoline derivatives by Friedel-Crafts cyclodehydration. The fluorine atom contributes to increased thermal stability, chemical resistance, and hydrophobicity of the resulting materials, making the compound valuable in the development of advanced materials and specialty coatings.

Major Market Participants

The global supply system for 2-amino-4′-fluorobenzophenone (CAS# 3800-06-4) features a pattern of “specialized pharmaceutical intermediate manufacturers, multinational research chemical distributors, and Chinese producers serving distinct market segments.” As a specialized fluorinated building block rather than a bulk commodity, the market is characterized by a moderate number of suppliers catering to pharmaceutical R&D, biotechnology, and materials science applications. Global market reports on 2-amino-4′-fluorobenzophenone provide comprehensive data on manufacturers, consumers, production situation, supply & demand analysis, price analysis, and import & export situation across Europe, Asia, North America, and Latin America.

In the global research and high-purity segment, key international suppliers include Tokyo Chemical Industry (TCI), offering the compound at >98.0% (GC)(T) purity with product code A2760, available in 1 g and 5 g quantities; Aladdin Scientific, offering 98% purity with triple ISO certification and COA/SDS available for all products; AKSci, offering 98% (HPLC) purity with product code F997; TargetMol, offering the compound at ≥99.52% purity for biochemical research applications; BOC Sciences, providing the compound as a building block with over 20,000 intermediates available from stock; and Chem-Impex International, offering the compound for pharmaceutical development research. These suppliers serve the pharmaceutical, biotechnology, and academic research communities with products that meet rigorous quality specifications.

In the industrial and large-scale production segment, Chinese manufacturers have emerged as significant players in the global supply chain. XinChem is a reliable manufacturer and supplier of high-purity 2-amino-4′-fluorobenzophenone from China, offering the compound with stringent quality standards for use in Pitavastatin synthesis, fluorescent probe development, and pharmaceutical intermediate applications. XinChem provides the compound as a light yellow to off-white crystalline powder with comprehensive quality documentation and flexible packaging options. Other Chinese suppliers include Shaanxi Dideu Chemical Co., Ltd. , Wuhan Huajiu Pharmaceutical Technology, Jinan Fanuo Chemical, Pusan Industry (Shaanxi), Wuhan Yuqing Jiaheng Pharmaceutical, Shaanxi Jinghe Pharmaceutical Technology, and Shenzhen Moke Biochemical Technology. Chinese suppliers offer the compound at various purity grades (typically 98–99%) and packaging options—from grams to multi-kilogram quantities—serving both domestic and export markets with competitive pricing. Production capacity from key Chinese manufacturers is estimated at 50 MT/month with loading port Shanghai. The compound is available at prices ranging from approximately RMB 30.9/g to RMB 240.9/25g for research quantities.

Regional Market Dynamics

The global 2-amino-4′-fluorobenzophenone 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, biotechnology, and materials science industries in these regions. Global market reports provide comprehensive data on regional markets including Europe, Asia, North America, and Latin America.

The Asia-Pacific region has emerged as a significant production hub for 2-amino-4′-fluorobenzophenone, 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 biotechnology industries. Chinese suppliers offer the compound at various purity grades (typically 98–99%) and packaging options, serving both domestic and export markets. The growing pharmaceutical R&D, Pitavastatin production, and fluorescent probe development sectors in China, Japan, South Korea, and India continue to drive regional consumption growth. TCI Chemicals maintains inventory in Japan and China, with the ability to ship from Shanghai and Tianjin warehouses.

North America remains a key market for high-purity and research-grade 2-amino-4′-fluorobenzophenone, 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 fluorinated building blocks for drug discovery and development. TCI America, AK Scientific, and BOC Sciences serve the North American market with extensive distribution networks. 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, including REACH registration, and a strong focus on quality and sustainability in pharmaceutical and chemical research. European pharmaceutical companies, biotechnology firms, and research institutions demand high-purity fluorinated building blocks with comprehensive documentation. CymitQuimica, Fluorochem, and other distributors serve the European market with in-stock availability.

Japan represents a specialized market where 2-amino-4′-fluorobenzophenone is supplied by TCI Chemicals and other distributors for pharmaceutical research, Pitavastatin intermediate production, and fluorescent probe development applications.

Regulatory and Safety Considerations

As a research chemical, pharmaceutical intermediate, and fluorinated building block, 2-amino-4′-fluorobenzophenone (CAS# 3800-06-4) 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-Amino-4′-fluorobenzophenone is classified with the signal word ”Warning” . Hazard statements include H315 (Causes skin irritation), H319 (Causes serious eye irritation), and H335 (May cause respiratory irritation). Precautionary statements include P261 (Avoid breathing dust/fume/gas/mist/vapours/spray), P264 (Wash skin thoroughly after handling), P280 (Wear protective gloves/protective clothing/eye protection/face protection), P302+P352 (IF ON SKIN: Wash with plenty of water), P305+P351+P338 (IF IN EYES: Rinse cautiously with water for several minutes; remove contact lenses if present and easy to do; continue rinsing), P332+P313 (If skin irritation occurs: Get medical advice/attention), and P337+P313 (If eye irritation persists: Get medical advice/attention). The compound is classified as an irritant and is air-sensitive, requiring storage under argon to prevent oxidative degradation. The WGK Germany classification is 3 (high hazard to water).

Storage and stability: 2-Amino-4′-fluorobenzophenone should be stored under argon in a cool, dark place (recommended below 15°C) to prevent oxidative degradation. For long-term storage, the powder is stable for 3 years at -20°C. The compound is air-sensitive and should be handled under inert atmosphere.

Regulatory compliance: In the European Union, the compound must comply with REACH registration requirements for import and use. Manufacturers and suppliers must provide comprehensive Safety Data Sheets (SDS) and maintain appropriate documentation. In the United States, 2-amino-4′-fluorobenzophenone 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.

Transport information: 2-Amino-4′-fluorobenzophenone 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 HS code for the compound is 2922.39-000 for Japan exports.

Environmental considerations: As a fluorinated aromatic compound, 2-amino-4′-fluorobenzophenone requires responsible handling and disposal. The compound is not classified as a persistent, bioaccumulative, and toxic (PBT) substance, but appropriate waste management protocols should be implemented to minimize environmental impact. The development of greener synthesis methods—including routes from phthalimide with reported yields of 85–91% and routes from o-nitrotoluene using environmentally friendly starting materials—is an ongoing focus in the industry.

Future Outlook

The market outlook for 2-amino-4′-fluorobenzophenone is positive, supported by several key growth drivers across its major application segments. While the compound remains a relatively specialized fluorinated building block, its strategic role as the key intermediate for Pitavastatin and its utility in fluorescent probe development position it for steady growth in the coming years. The global market for fluorinated pharmaceutical intermediates—driven by increasing demand for statins, oncology therapeutics, and diagnostic probes—is projected to maintain steady growth through the forecast period.

Key growth drivers include:

1. Expansion of the Pitavastatin market: The continued global demand for Pitavastatin—a potent, third-generation statin with favorable safety and drug interaction profiles—drives demand for the key intermediate 2-amino-4′-fluorobenzophenone. Rising prevalence of hypercholesterolemia and cardiovascular disease, particularly in aging populations, supports sustained demand.
2. Growth in fluorescent probe and bioimaging technologies: The expanding market for fluorescent probes and biological imaging tools—particularly for DNA/RNA detection, live-cell imaging, and diagnostic assays—creates new opportunities for the compound and its derivatives.
3. Increasing demand for fluorinated pharmaceutical intermediates: The growing emphasis on metabolic stability and bioavailability in drug design drives demand for regioisomer-specific fluorinated building blocks that enable precise control over molecular properties.
4. Expansion of pharmaceutical R&D in Asia: The growth of pharmaceutical R&D and API manufacturing in China and India—driven by increasing investment in generic drug production and innovative drug discovery—supports demand for high-quality pharmaceutical intermediates.
5. Advantages of orthogonal synthesis: The compound’s ability to serve as a versatile scaffold for constructing complex therapeutic molecules through Friedel-Crafts acylation, cyclodehydration, and other transformations makes it increasingly valuable in modern synthetic chemistry.

Challenges and considerations:

• Regulatory compliance: Increasingly stringent pharmaceutical and chemical regulations may require ongoing investment in quality systems and documentation.
• Air sensitivity: The compound’s air-sensitive nature requires storage under inert atmosphere, which may increase handling and logistics costs.
• Competition from alternative building blocks: The market faces competition from other fluorinated benzophenones and alternative synthetic routes to Pitavastatin intermediates.
• Limited scale: As a relatively specialized compound, the market for 2-amino-4′-fluorobenzophenone is smaller than that of commodity chemicals.
• Handling requirements: The compound’s irritant classification (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 regioisomeric purity, low moisture content, 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, biotechnology, and materials science applications will be well-positioned to capture growing demand.

Shanghai XinChem Co., Ltd. (XinChem)

As a world-leading supplier of organic chemicals and fluorinated building blocks, Shanghai XinChem Co., Ltd. (XinChem) is dedicated to meeting the innovative needs of the pharmaceutical, biotechnology, and fine chemical industries. Leveraging extensive experience and advanced manufacturing capabilities, XinChem provides high-quality 2-Amino-4′-fluorobenzophenone (CAS# 3800-06-4) 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 fluorinated benzophenone 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-amino-4′-fluorobenzophenone products. The production process incorporates established synthetic routes—including the Friedel-Crafts acylation of phthalimide with fluorobenzene followed by Hofmann degradation (reported yields of 85–91%) and the environmentally friendly o-nitrotoluene route—enabling the delivery of products with purity ≥98% (GC and non-aqueous titration) to meet diverse application requirements. Strict process control ensures consistent regioisomeric purity, minimal impurities, and batch-to-batch reproducibility, providing customers with reliable performance in Pitavastatin synthesis, fluorescent probe development, and pharmaceutical intermediate 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 (GC and non-aqueous titration), melting point (127.0–131.0°C), and impurity profiles. This commitment to quality ensures that XinChem’s 2-amino-4′-fluorobenzophenone meets the stringent requirements of pharmaceutical R&D, biotechnology research, and materials science applications.

2. Product Advantages

High Purity and Consistent Quality
XinChem offers 2-amino-4′-fluorobenzophenone with purity ≥98% (GC and non-aqueous titration), ensuring optimal performance in Pitavastatin synthesis, fluorescent probe development, and pharmaceutical intermediate applications. The product’s high purity and regioisomeric specificity minimize the risk of unwanted side reactions and impurities, making it suitable for demanding applications in drug discovery, bioimaging, and advanced materials.

Comprehensive Specifications
Key specifications include:

• Molecular Formula: C₁₃H₁₀FNO
• Molecular Weight: 215.22 g/mol
• CAS Number: 3800-06-4
• Synonyms: (2-Aminophenyl)(4-fluorophenyl)methanone; 2-Amino-4′-fluorodiphenylmethanone
• MDL Number: MFCD06658166
• Appearance: Light yellow to off-white crystalline powder
• Purity: ≥98.0% (GC) / ≥98.0% (non-aqueous titration)
• Melting Point: 124–131°C (literature 127–131°C)
• Solubility: Chloroform (soluble); DMSO (25 mg/mL); low solubility in water
• Storage: Under argon, cool and dark place (recommended below 15°C); powder stable for 3 years at -20°C

Flexible Packaging Solutions
XinChem provides a range of packaging options to accommodate diverse customer needs, from laboratory-scale quantities (1 g, 5 g, 10 g, 25 g, 100 g) to industrial-scale packaging (500 g, 1 kg, 25 kg/drum) and bulk shipments. Customized packaging solutions are available upon request, ensuring safe handling, storage, and transportation with appropriate protection from air and moisture.

3. Application Fields

As a versatile regioisomer-specific fluorinated benzophenone building block, 2-Amino-4′-fluorobenzophenone (CAS# 3800-06-4) exhibits wide application value across multiple industries:

Pharmaceutical Synthesis and Drug Intermediates:

• Key intermediate for Pitavastatin (Livalo®), a third-generation HMG-CoA reductase inhibitor for hypercholesterolemia and cardiovascular disease prevention
• Precursor for p-fluorobenzoyl chloride
• Building block for anti-cancer agents and other therapeutic drugs
• Intermediate for anti-inflammatory compounds targeting key cytokines and enzymes
• Reference standard for API quality control and analytical method validation

Fluorescent Probes and Biochemical Research:

• Fluorescent probe for DNA and RNA detection
• Fluorescence derivatization reagent for aromatic aldehydes in liquid chromatography
• Tool for live-cell imaging and diagnostic assays

Dyes, Pesticides, and Specialty Chemicals:

• Intermediate for dyes and pesticides
• Friedel-Crafts acylation reagent for quinoline derivative synthesis
• Building block for specialty materials with enhanced thermal stability and chemical resistance

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 handling air-sensitive compounds, 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 protection from air and moisture for product stability.

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 fluorinated building block synthesis and supply.
• Quality: Rigorous quality control, high purity (≥98%), regioisomeric specificity, 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