5-Bromo-4-fluoro-1H-indazole (CAS 1082041-85-7): Core Value and Industrial Supply Advantages of High-end Pharmaceutical Intermediates

As a key pharmaceutical intermediate in the field of heterocyclic compounds, 5-Bromo-4-fluoro-1H-indazole (CAS NO. 1082041-85-7) has become a core basic raw material in pharmaceutical R&D and organic synthesis due to its unique molecular structure and excellent chemical activity, and is widely used in the synthesis and R&D of innovative drugs for anti-tumor, anti-inflammatory, neurological diseases and other indications. Shanghai Lizhuo Pharmaceutical Technology Co., Ltd.  has been deeply engaged in the R&D and production of high-end pharmaceutical intermediates for many years, realizing the large-scale and high-purity industrial production of 5-Bromo-4-fluoro-1H-indazole, and providing stable and high-quality product supply and customized solutions for pharmaceutical enterprises and R&D institutions worldwide.

I. Analysis of Core Product Identification and Physicochemical Properties

1. Basic Product Identification Information

Chinese Name: 5-溴-4-氟-1H-吲唑English Name: 5-Bromo-4-fluoro-1H-indazoleCAS Registry Number: 1082041-85-7Molecular Formula: C7H4BrFN2Molecular Weight: 215.02Molecular Structure: It contains an indazole parent nucleus (a bicyclic structure fused by a benzene ring and a pyrazole ring), with the halogen modification characteristics of bromine substitution at the 5-position and fluorine substitution at the 4-position. Its InChI is 1S/C7H4BrFN2/c8-5-1-2-6-4(7(5)9)3-10-11-6/h1-3H,(H,10,11), and SMILES is N1C2=C(C(F)=C(Br)C=C2)C=N1.

2. Key Physicochemical Properties

5-Bromo-4-fluoro-1H-indazole is an off-white to brown solid powder, a thermodynamically stable 1H-indazole tautomer, with typical chemical characteristics of halogenated heterocyclic compounds. Its core physicochemical parameters are as follows:

• Density: 1.861±0.06 g/cm³ (predicted value), with a compact molecular structure and solubility compatible with most organic synthesis solvents;
• Boiling Point: 332.2±22.0 ℃ (predicted value), with excellent thermal stability and tolerance to conventional organic synthesis reaction temperatures;
• Acid Dissociation Constant (pKa): 11.95±0.40 (predicted value), with weak basic characteristics, which can form stable complexes with acidic reagents for easy reaction regulation;
• Storage Conditions: Sealed at room temperature, stored in a dark and dry place, non-hygroscopic, non-flammable and non-explosive, with high safety in transportation and storage;
• Chemical Activity: Bromine and fluorine halogen substituents have strong electronic effects and can undergo nucleophilic substitution, cross-coupling and other reactions. They are key sites for the structural modification of the indazole parent nucleus, providing abundant derivatization possibilities for the subsequent synthesis of drug molecules.

3. Purity and Quality Standards

The industrial-grade 5-Bromo-4-fluoro-1H-indazole produced by our company has a purity of ≥98%, and the high-end customized grade product can reach a purity of more than 99.5%, with a single impurity content of ≤0.1% and no heavy metal residues (Pb, As, Hg, etc. ≤10ppm). It complies with the international pharmacopoeia standards such as USP, EP and CP, meeting the quality requirements of drug R&D and large-scale production.

II. Core Application Fields and Market Development Prospects of the Product

As a core pharmaceutical intermediate of halogenated indazole derivatives, 5-Bromo-4-fluoro-1H-indazole endows it with irreplaceability in organic synthesis and drug R&D due to its unique molecular structure. The indazole parent nucleus is an “advantageous skeleton” in the field of medicinal chemistry, and drug molecules with various biological activities can be synthesized through structural modification. At present, the product has become an important raw material in the global innovative drug R&D and fine chemical industry.

1. Core Application Fields

(1) R&D and Production of Innovative Drugs

It is a key intermediate for the synthesis of innovative drugs for major diseases such as anti-tumor, anti-inflammatory, neurological diseases and diabetes. The indazole parent nucleus can synthesize a variety of targeted drug molecules through halogen substitution and ring modification, such as SHP2 inhibitors, EP3 receptor antagonists, TRPV1 receptor blockers, etc., which are widely used in the R&D of therapeutic drugs for lung cancer, breast cancer, rheumatoid arthritis, Parkinson’s disease and other diseases. For example, the EP3 receptor antagonist synthesized based on this intermediate can effectively improve the oral glucose tolerance of patients with type 2 diabetes, becoming an important direction for the R&D of metabolic disease drugs.

(2) Organic Synthesis and Molecular Building Block Preparation

As a high-end organic synthesis molecular building block, it can realize the further functional modification of the indazole parent nucleus through cross-coupling reactions such as Suzuki and Heck to prepare 4-fluoro-5-substituted indazole derivatives, which are widely used in fine chemical industry, new material synthesis and other fields. At the same time, its halogen-substituted structural characteristics provide a basis for the structural optimization of heterocyclic compounds, making it an important research raw material in the fields of medicinal chemistry and organic synthesis.

(3) Pharmaceutical R&D Reagents and Laboratory Research

It provides high-quality R&D reagents for universities, research institutes and pharmaceutical R&D enterprises worldwide, used for drug molecular design, activity screening, structure-activity relationship research, etc. It is a common basic raw material in pharmaceutical R&D laboratories and provides technical support for the early R&D of innovative drugs.

2. Market Development Prospects and Demand Trends

With the continuous warming of global innovative drug R&D, the application value of indazole heterocyclic compounds as an “advantageous drug skeleton” is constantly improving, driving the continuous growth of market demand for 5-Bromo-4-fluoro-1H-indazole. The core market characteristics are as follows:

1. Steady growth of global demand: The R&D pipeline of innovative drugs in anti-tumor, anti-inflammatory, neurological diseases and other fields is continuously enriched. The demand of international large pharmaceutical enterprises (such as GSK, Pfizer, Abbott, etc.) for high-end halogenated indazole intermediates is increasing year by year, and the global market compound annual growth rate remains above 15%;
2. Huge potential of the domestic market: China’s pharmaceutical industry is transforming to “innovation-driven”, the R&D investment of local pharmaceutical enterprises in innovative drugs is continuously increasing. At the same time, China has become an important production base of pharmaceutical intermediates in the world, and the demand for localized supply of high-purity 5-Bromo-4-fluoro-1H-indazole is urgent;
3. High-end and customized becoming the mainstream: Pharmaceutical enterprises have increasingly high requirements for the purity, quality stability and customized synthesis capacity of pharmaceutical intermediates. The market share of high-purity (≥99%) and customized derivative products is continuously increasing, and low-end products are gradually eliminated;
4. Green production becoming an industry trend: The global chemical industry is transforming to green, environmental protection and low carbon, and production enterprises with green synthesis processes and waste treatment capacity up to standard will occupy a dominant position in the market.

At present, the market demand for 5-Bromo-4-fluoro-1H-indazole is mainly concentrated in North America, Europe, China, India and other developed pharmaceutical industry regions. Among them, the large-scale production demand of pharmaceutical enterprises and the small-batch customized demand of R&D institutions complement each other, forming a diversified market demand structure.

III. Core Competitive Advantages and Industrial Capacity Guarantee of Our Company’s Products

Shanghai Lizhuo Pharmaceutical Technology Co., Ltd.  focuses on the R&D, production and sales of high-end pharmaceutical intermediates and fine chemical products, and has been deeply engaged in the field of heterocyclic compounds for many years. It has a R&D and production team composed of senior chemical engineers and pharmaceutical experts, with the full-process capability from laboratory small-scale test, pilot scale-up to industrial large-scale production. For the production of 5-Bromo-4-fluoro-1H-indazole (CAS 1082041-85-7), our company has formed four core advantages of technology, quality, capacity and service, providing stable and high-quality product supply for global customers.

1. Core Technical Advantage: Independently Developed Green Synthesis Process

Our company has broken through the bottleneck of the traditional synthesis process and independently developed the green synthesis process of 5-Bromo-4-fluoro-1H-indazole. The product is synthesized by an optimized process of diazotization, cyclization and extraction purification with 4-bromo-3-fluoro-2-methylaniline as the raw material, which has significant advantages over the traditional process:

• High Yield: By optimizing the reaction conditions and purification process, the total product yield is increased to more than 70%, far exceeding the industry average of 63%, effectively reducing the production cost;
• Environmental Protection: Low-toxic and recyclable solvents are adopted to reduce the use of heavy metal reagents. The discharge of three wastes (waste gas, waste water and industrial residue) is reduced by 60% compared with the traditional process. Waste water and waste gas are discharged up to standard after treatment, complying with national environmental protection standards and the global development trend of green chemical industry;
• Stable Process: Realize precise temperature control and automatic regulation of the reaction process, avoid side reactions, ensure high quality stability between product batches, and the purity fluctuation is ≤0.5%;
• Strong Scalability: The process route can realize seamless scale-up from kilogram level to ton level without re-optimizing process parameters, providing technical guarantee for large-scale production.

At the same time, our company has a number of core patents for the synthesis of heterocyclic compounds. The R&D team can provide customized synthesis services of 5-Bromo-4-fluoro-1H-indazole derivatives according to customer needs to meet the personalized needs of different customers.

2. Quality Advantage: Full-process Quality Control in Line with International Standards

Our company has established a full-process Quality Management System (QMS) from raw material procurement to finished product delivery, and strictly controls the entire production process of 5-Bromo-4-fluoro-1H-indazole with reference to ISO9001 and GMP quality management standards:

• Raw Material Control: Select high-quality raw material suppliers and conduct full-item inspection on raw materials to ensure the raw material purity ≥99% without impurity interference;
• Process Control: Set up multiple quality inspection nodes in the production process, and use advanced testing equipment such as High Performance Liquid Chromatography (HPLC), Gas Chromatography (GC) and Nuclear Magnetic Resonance (NMR) to monitor the reaction process and product purity in real time;
• Finished Product Inspection: Conduct full-item index testing on finished products before delivery, including purity, melting point, boiling point, heavy metal residue, moisture, ash content, etc., to ensure that each batch of products meets customer requirements and international pharmacopoeia standards, and provide a complete test report;
• Quality Traceability: Establish a product batch traceability system, each batch of products has a unique batch number, which can trace the raw material source, production process, test data and delivery information, providing quality assurance for customers.

3. Capacity Advantage: Large-scale Production Base with Multi-line Layout to Guarantee Supply

Our company has a modern pharmaceutical intermediate production base equipped with multiple special production lines for 5-Bromo-4-fluoro-1H-indazole, realizing large-scale and continuous production of the product, with industry-leading capacity guarantee capability:

• Core Capacity: At present, the annual production capacity of 5-Bromo-4-fluoro-1H-indazole of our company reaches 50 tons, which can meet the large-scale production needs of large pharmaceutical enterprises;
• Flexible Production: Equipped with small-scale and pilot production lines, it can meet the small-batch (100g-10kg) customized needs of R&D institutions and small and medium-sized enterprises with a short delivery cycle;
• Capacity Reserve: The company has completed the capacity expansion plan, and the annual production capacity will be increased to 100 tons after the commissioning of the second-phase production line, further improving the global market supply capacity;
• Warehousing and Logistics: It has a professional dangerous goods storage warehouse with constant temperature, dry and dark storage facilities, and sufficient product inventory; Cooperate with world-renowned logistics enterprises to realize rapid domestic delivery and international sea and air transportation, with a 100% on-time delivery rate.

4. Service Advantage: One-stop Solution with Global Localized Service

Adhering to the customer-centric service concept, our company provides global customers with a one-stop solution from product supply to technical support:

• Customized Service: We can provide products with different purities and specifications according to customer needs, and at the same time provide technical services such as customized synthesis of derivatives and process optimization;
• Technical Support: We have a professional technical service team to provide customers with technical support such as product application guidance, reaction process optimization and quality problem solving, with 7×24-hour online response;
• Global Layout: Set up overseas offices in North America, Europe, Southeast Asia and other regions to realize global localized services, providing fast sample delivery, order delivery and technical support for overseas customers;
• Long-term Cooperation: Establish long-term strategic cooperative partnerships with many well-known domestic and foreign pharmaceutical enterprises and R&D institutions, formulate personalized supply plans according to customer needs, and ensure long-term and stable supply.

IV. Enterprise Strength and Future Development

As a leading enterprise in the field of high-end pharmaceutical intermediates, Shanghai Lizhuo Pharmaceutical Technology Co., Ltd. has always adhered to the development philosophy of “technological innovation, quality first, green development and win-win cooperation”, and deeply engaged in the fields of heterocyclic compounds and halogenated intermediates, with a complete R&D, production, sales and service system. The company has successively passed the ISO9001 Quality Management System, ISO14001 Environmental Management System and OHSAS18001 Occupational Health and Safety Management System certification, and a number of products have been highly recognized by international customers.

For 5-Bromo-4-fluoro-1H-indazole (CAS 1082041-85-7) and indazole intermediate products, our company will continue to increase R&D investment, further optimize the synthesis process, improve product quality and capacity, and at the same time expand the product derivative system, develop more high value-added indazole derivative products to meet the global demand for innovative drug R&D and production.

In the future, the company will continue to take technological innovation as the core and the global market as the guide, constantly enhance the core competitiveness of the enterprise, strive to become a core supplier of high-end pharmaceutical intermediates in the world, and contribute to the development of the global pharmaceutical industry. If you have procurement needs or customized service needs for 5-Bromo-4-fluoro-1H-indazole (CAS 1082041-85-7) products, please contact us through our official website ), and we will provide you with high-quality products and professional services!