(2R)-2-Ethyl-2,3-dihydro-6-(trifluoromethyl)quinolin-4(1H)-one (CAS: 952582-00-2) is a chiral, fluorine-containing fused heterocyclic compound belonging to the dihydroquinolin-4(1H)-one family, with the molecular formula C₁₂H₁₂F₃NO and a molecular weight of 243.23 g/mol. Its core structure — a 2,3-dihydroquinolin-4(1H)-one scaffold featuring an ethyl substituent at the chiral 2-position and a trifluoromethyl group at the 6-position — provides a conformationally rigid pharmacophore platform highly suitable for targeted drug design. The presence of the chiral (2R)-center and the powerful electron-withdrawing trifluoromethyl substituent (-CF₃) combine to impart enhanced metabolic stability, improved binding affinity to biological targets, and favorable physicochemical properties for oral bioavailability.
This compound has been identified as a key intermediate for CRTH2 (chemoattractant receptor-homologous molecule expressed on Th2 cells) antagonists. CRTH2 is a high-affinity receptor for prostaglandin D₂ (PGD₂), a key mediator involved in type 2 inflammatory responses. Activation of CRTH2 by PGD₂ plays a critical role in the recruitment of Th2 cells, eosinophils, and basophils to inflamed tissues in allergic asthma, atopic dermatitis, allergic rhinitis, and other eosinophilic inflammatory disorders. Antagonists of the CRTH2 receptor, therefore, represent an important and actively pursued therapeutic strategy for the treatment of these allergic and inflammatory diseases. The trifluoromethyl-substituted dihydroquinolinone scaffold has been explored in the development of potent and selective CRTH2 antagonists, with several compounds advancing into clinical trials. The global prostaglandin D2 receptor 2 market, which encompasses CRTH2 antagonists, was valued at USD 102 million in 2023 and is projected to reach USD 178.9 billion by 2030, growing at a CAGR of 25%.
In addition to its role as a key intermediate for CRTH2 antagonists, the dihydroquinolin-4(1H)-one scaffold has been reported as a promising template for anti-tumor, antiviral, and central nervous system drugs. The compound also serves as a core structural unit in the optimization of lead compounds for kinase inhibitors, 5-HT receptor modulators, or PD-L1 inhibitors. The unique bicyclic structure allows for optimization of anti-proliferative activity while maintaining selectivity. Furthermore, the trifluoromethylquinoline motif is increasingly recognized as a privileged structure in the design of dual-target therapeutic agents spanning oncology, inflammation, and central nervous system disorders. The compound is therefore positioned at the intersection of several high-value drug discovery programs: anti-inflammatory, anti-allergic, anti-cancer, and antiviral.
Major Market Participants
The global supply system for (2R)-2-ethyl-2,3-dihydro-6-(trifluoromethyl)quinolin-4(1H)-one (CAS: 952582-00-2) features a pattern of “specialized fine chemical and pharmaceutical intermediate manufacturers, primarily in China, India, Europe, and North America, serving both small-scale R&D and large-scale production.” The compound is generally supplied as a white to off-white crystalline solid with purity ranging from 97% to ≥98% by HPLC. The compound has a predicted boiling point of 323.1±42.0 °C and a density of 1.216±0.06 g/cm³. Storage is recommended at 2-8°C in a dry, dark, and sealed environment.
Shanghai XinChem Co., Ltd. (XinChem) has established a reliable, quality-controlled supply chain for high-purity (2R)-2-ethyl-2,3-dihydro-6-(trifluoromethyl)quinolin-4(1H)-one (CAS 952582-00-2). Our product is manufactured under strict quality management, achieving consistent purity (≥98-99% by HPLC) with low residual solvents and low heavy metals, fully complying with pharmaceutical intermediate standards. It is an ideal building block for CRTH2 antagonists, kinase inhibitors, and other heterocyclic drug candidates.
Regional Market Dynamics
Global demand for (2R)-2-ethyl-2,3-dihydro-6-(trifluoromethyl)quinolin-4(1H)-one shows regional differentiation: “Asia-Pacific dominates production, North America and Europe lead in high-purity R&D and pharmaceutical applications, and Latin America & Middle East/Africa follow as emerging growth markets.” The CRTH2 antagonist market is experiencing significant growth across all major regions, driven by the rising prevalence of allergic and inflammatory diseases.
Asia-Pacific, led by China and India, is the world’s largest producer of heterocyclic intermediates and a rapidly growing consumer. China’s integrated chemical manufacturing base enables cost-effective production of complex heterocycles, with manufacturers offering high-purity material at competitive prices. India‘s expanding generic pharmaceutical and contract research organization (CRO) sector also drives significant volume demand.
North America (United States and Canada) and Europe (Germany, Switzerland, United Kingdom, France) together account for the largest share of high-purity R&D and commercial consumption (≥99%), driven by the highest concentration of CRTH2-targeting drug discovery programs, anti-inflammatory drug development, and advanced agrochemical innovation centers. 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 and related substances by HPLC-UV), and cGMP documentation for pharmaceutical use.
Regulatory and Environmental Considerations
As a pharmaceutical intermediate, (2R)-2-ethyl-2,3-dihydro-6-(trifluoromethyl)quinolin-4(1H)-one (CAS 952582-00-2) is subject to chemical control regulations and, when intended for drug use, to GMP guidelines. The compound has no clear GHS classification, but fluorinated organic compounds usually need to avoid inhaling dust, and it is recommended to wear protective equipment during operation.
In the European Union, the compound 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 pharmaceutical API use, 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) and requires safety production licenses for manufacturing facilities.
Environmentally, as with all fluorinated organic compounds, responsible handling and disposal are essential to prevent environmental contamination. Manufacturing generates solvent-containing waste streams requiring proper treatment.
Future Outlook
The market outlook for (2R)-2-ethyl-2,3-dihydro-6-(trifluoromethyl)quinolin-4(1H)-one is tied to four core drivers: (1) the sustained growth of the global CRTH2 antagonist market — projected to reach USD 178.9 billion by 2030 at a CAGR of 25%; (2) the continued expansion of targeted kinase inhibitor pipelines for oncology, anti-inflammatory, and CNS disorders; (3) the rapid growth of Asian CRO/CDMO sectors supplying intermediates to global pharmaceutical companies; and (4) the privileged position of the dihydroquinolinone scaffold in fragment-based drug discovery (FBDD) programs.
Enterprises should focus on securing high-purity chiral production capabilities, maintaining rigorous impurity documentation for pharmaceutical regulatory filings, and building long-term supply partnerships with API manufacturers, CROs, and research institutions.
Shanghai XinChem Co., Ltd. (XinChem)
As a world-leading supplier of pharmaceutical intermediates and heterocyclic building blocks, Shanghai XinChem Co., Ltd. (XinChem) has always focused on the innovative needs of the targeted therapeutics, anti-inflammatory drug discovery, and respiratory API industries. Relying on core advantages in chiral heterocyclic synthesis, purification, and quality assurance, we provide high-quality (2R)-2-ethyl-2,3-dihydro-6-(trifluoromethyl)quinolin-4(1H)-one (CAS 952582-00-2) to global customers.
1. Technical Advantages
- High Purity & Chiral Consistency: Our product achieves purity ≥98-99% (by HPLC), white to off-white crystalline solid, molecular weight 243.23 g/mol, molecular formula C₁₂H₁₂F₃NO, and moisture <0.5% (KF titration). The (2R)-chirality is preserved throughout synthesis and verified by chiral HPLC.
- Low Impurity Profile: Strict control of residual solvents (<0.5% total), heavy metals (≤10 ppm, ICH Q3D compliant), and related substances by HPLC-UV.
- Batch-to-Batch Uniformity: Rigorous analytical testing (HPLC, NMR, LC-MS, heavy metals by ICP-MS, residual solvents by GC-headspace) guarantees consistent quality.
2. Product Advantages
- Potent CRTH2 Antagonist Scaffold: The trifluoromethyl-substituted dihydroquinolinone core serves as a key building block for CRTH2 antagonist development.
- Privileged Heterocyclic Framework: Widely employed in medicinal chemistry campaigns targeting respiratory and allergic diseases, oncology, and CNS disorders.
- Flexible Packaging Options: 5g, 10g, 25g, 50g, 100g, 500g, 1kg glass bottles/HDPE containers (R&D/pilot); 5kg, 10kg, 25kg fiber drums (industrial). Full custom packaging available.
- Reliable Supply Chain: Annual capacity 50-200kg, with dedicated temperature-controlled warehousing (2-8°C, light-protected, sealed containers) and just-in-time delivery capabilities.
3. Application Fields
- Pharmaceutical Intermediates: Key building block for CRTH2 antagonists for allergic asthma, atopic dermatitis, and allergic rhinitis; kinase inhibitors; anti-tumor, antiviral, and CNS agents.
- CRO/CDMO Custom Synthesis: Essential custom-synthesized intermediate for medicinal chemistry outsourcing, hit-to-lead optimization, and preclinical toxicology studies.
- Drug Discovery Library Construction: Enabling building block for fragment-based drug discovery (FBDD), structure-activity relationship (SAR) campaigns, and high-throughput screening.
4. Service Support
Our technical team provides full impurity profiling (chiral purity by chiral HPLC, 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 trifluoromethyl quinolinone derivatives, cold-chain logistics, and just-in-time delivery.
5. Why Choose XinChem
- Professionalism: 20+ years in the pharmaceutical intermediate and heterocyclic synthesis industry.
- Flexibility: Tailored to customer purity specifications, chiral purity documentation, packaging sizes, and regulatory documentation requirements.
- Cost-effectiveness: High purity at competitive industrial pricing.
Contact us now to start cooperation!
Website: www.xinchem.com
Email: sales1@xinchem.com
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Post time: Jul-05-2026