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4-Bromo-3-fluoro-2-methylaniline (CAS 127408-03-1) High-Purity Pharmaceutical Intermediate Full Introduction

In the industrial chain of modern fine chemicals and new drug R&D, bromo-fluoro substituted methylaniline aromatic intermediates serve as core raw materials for constructing targeted drugs, novel agrochemicals and organic synthetic building blocks. With its unique tri-substituted benzene ring structure, 4-Bromo-3-fluoro-2-methylaniline (CAS No.127408-03-1) carries multiple active functional groups including amino, fluorine, bromine and methyl groups. It has become a high-end aromatic amine intermediate with steadily rising demand in new drug research and organic catalytic synthesis in recent years. As a regular mass producer of this product, Shanghai Lizhuo Pharmaceutical can supply standard samples with purity above 97%, supporting trial sample application and stable ton-level bulk supply. This article comprehensively analyzes the product from basic information, physicochemical parameters, application sectors, market trends, production capacity and core advantages of our factory, providing professional references for procurement by pharmaceutical enterprises, chemical R&D institutions and fine chemical manufacturers.

I. Basic Name, CAS Number and Accurate Physicochemical Parameters of 4-Bromo-3-fluoro-2-methylaniline (Data sourced from product detail page with zero error in parameters)

1. Standard Chemical Nomenclature System

Common Chinese Name:4-Bromo-3-fluoro-2-methylaniline

Standard English Name: 4-Bromo-3-fluoro-2-methylaniline Exclusive CAS Registry Number: 127408-03-1. This number acts as the sole global identification code for chemical and pharmaceutical procurement, adopted for customs clearance, R&D declaration and reagent filing without risks of number duplication and confusion.

2. Fundamental Molecular Structural Parameters

Molecular Formula: C₇H₇BrFN Exact Molecular Weight: 204.04 Advantages of Molecular Structure: The benzene ring is tetra-substituted with ortho-methyl, 3-fluoro, 4-bromo and 1-amino groups. Fluorine atoms improve molecular lipophilicity and metabolic stability; bromine atoms function as key leaving sites for Suzuki coupling, Buchwald amination and Heck reactions; amino groups can undergo diazotization, acylation, alkylation and cyclization reactions. Multiple functional groups endow this compound with strong derivatization capacity for synthesis, making it an irreplaceable high-end synthetic building block compared with ordinary mono-substituted anilines.

3. Complete Physicochemical Performance Indicators (Enterprise measured data plus professional predictive data)

1. Appearance: Pink crystalline solid, easy to subpackage and feed without viscous oily impurities, convenient for lab-scale trial and industrial mass feeding;

2. Standard Product Purity: Stably mass-produced specification ≥97%, higher purification grades available on demand with strictly controlled impurities and excessive isomer content;

3. Boiling Point: 244.5±35.0 °C (predicted value), featuring favorable high-temperature stability and good compatibility with distillation purification processes;

4. Density: 1.589±0.06 g/cm³. This high-density halogen-substituted aromatic amine avoids stratification and sedimentation during storage;

5. Storage Conditions: Sealed storage away from light at 2-8°C. Long-term exposure to light and high temperature will trigger oxidation and discoloration of amino groups, and low-temperature light-proof storage can extend the shelf life to 2 years;

6. Note on Missing Parameters: MDL number, EINECS number, melting point, refractive index and flash point have no authoritative measured public data, uniformly marked N.A. in procurement and experimental reports to prevent R&D and production accidents caused by falsified parameters.

4. Brief Chemical Properties

This substance belongs to aromatic primary amines and can form salts with strong acids, with amino groups showing typical nucleophilic reactivity. The strong electron-withdrawing effect of fluorine atoms on the benzene ring regulates electron cloud distribution on the ring, delivering high selectivity at bromine sites and fewer reaction byproducts, which greatly reduces purification costs for downstream synthesis. Compared with ordinary methylanilines without fluorine or bromine, intermediates of this type can raise the yield of target synthetic products by more than 20%, becoming the preferred starting material for innovative high-end drug research.

II. Application Sectors and Industrial Market Analysis of 4-Bromo-3-fluoro-2-methylaniline

(I) Core Application Scenarios

1. Intermediate for Innovative Small-Molecule Drugs (Largest Downstream Market)

With continuous expansion of global targeted small-molecule drug R&D, fluoro-halo aromatic amines act as core synthetic units for kinase inhibitors, anti-inflammatory drugs and anti-tumor drug candidates. As a key starting material, 4-Bromo-3-fluoro-2-methylaniline is mainly applied in the synthesis of three categories of pharmaceuticals: First, targeted anti-tumor inhibitors: Synthesis of BTK, JAK, PI3K series small-molecule inhibitors. Heterocyclic pharmacophores are introduced via coupling at bromine sites, and fluorine atoms optimize cellular permeability of drugs, lower in-vivo metabolic clearance rate and extend drug half-life; Second, new non-steroidal anti-inflammatory drugs: Different from traditional ibuprofen and diclofenac, new-generation selective inflammatory pathway inhibitors widely adopt multi-substituted fluoro-bromoaniline skeletons with fewer side effects, whose market demand rises year by year; Third, anti-infective and antibacterial drugs: Construction of side chains for quinolone derivatives and novel heterocyclic antibacterial agents. Fluorine-containing structures can significantly boost bacteriostatic activity and reduce the emergence of drug-resistant strains.

In pharmaceutical synthetic routes, this product mainly participates in core procedures including diazotization, palladium-catalyzed cross-coupling, reductive cyclization and amide condensation. Innovative pharmaceutical enterprises, CRO R&D institutions and API manufacturers at home and abroad keep it in the regular list of R&D materials.

2. Intermediate for High-End Agrochemicals

Green low-residue pesticides represent the mainstream development trend of agricultural chemicals. Fluoro-halo aromatic herbicides, fungicides and insecticides feature low dosage, rapid degradation and high crop safety. 4-Bromo-3-fluoro-2-methylaniline can synthesize heterocyclic agricultural fungicides and selective gramineous herbicides, and active pesticide molecules are constructed by modifying amino and bromine sites. As China’s pesticide industry upgrades and outdated high-toxic aniline raw materials are phased out, procurement demand for high-end haloanilines grows steadily.

3. Scientific Research Reagents and Raw Materials for Catalytic Ligands in Organic Synthetic Chemistry

University chemistry labs, pharmaceutical R&D labs and new material research institutes purchase 97% purity of this product in large quantities for methodology research:

1. Model substrates for organic coupling reactions: Standard experimental raw materials for Suzuki-Miyaura, Ullmann and Buchwald-Hartwig amination reactions;

2. Building blocks for functional organic materials: Intermediates for liquid crystal monomers, organic optoelectronic materials and conjugated polymers. Fluoro-bromo substituted structures can adjust optoelectronic and heat-resistant properties of materials;

3. Precursors for chelating ligands: Derivatives to synthesize nitrogen-containing heterocyclic organophosphine ligands suitable for catalytic hydrogenation and asymmetric synthesis systems, matching with organophosphorus ligands such as 2-diphenylphosphinopyridine (CAS 37943-90-1).

4. Intermediate for Fine Dyes and Functional Pigments

Fluoro-aromatic dyes are characterized by light resistance, washing fastness and stable color. After diazotization, this product can be made into azo disperse dyes and textile functional pigments for high-grade chemical fiber and leather dyeing processes. The finished dyes deliver more than doubled weather resistance compared with ordinary aniline dyes.

(II) Current Status and Development Trend of the Global Market

Sustained expansion of global market demand The global CRO and CDMO outsourcing industries develop rapidly, with hundreds of new small-molecule drug candidates entering clinical trials every year. As customized intermediates, multi-substituted fluoro-bromoanilines maintain an annual compound growth rate of around 12%. European, American, Japanese and South Korean pharmaceutical R&D enterprises have strong import demand for high-purity, batch-stable 4-Bromo-3-fluoro-2-methylaniline. Qualified mass production manufacturers are scarce domestically, leading to a long-term supply shortage.

Prominent advantages of domestic industrial chains China boasts a complete supporting system for fine chemicals, with superior raw material costs and delivery cycles compared with overseas suppliers. An increasing number of foreign pharmaceutical and chemical enterprises turn to China for procurement of high-end haloaniline intermediates. Nevertheless, most small-scale workshops in the industry can only produce low-purity crude products with excessive impurities and unstable batches, failing to meet GMP standards for pharmaceutical raw materials. Compliant large-scale mass production manufacturers hold strong market competitiveness.

Demand for high-quality products driven by procurement pain points Currently, low-cost crude products in the market generally have three major drawbacks: purity below 95%, excessive isomer impurities and easy oxidation discoloration during storage, which directly reduce the yield of downstream pharmaceutical synthesis and cause impurity standards to fail drug declaration. Standardized products with ≥97% high purity, stable batches and standardized light-proof low-temperature storage have become rigid procurement demands for pharmaceutical enterprises, and source manufacturers with long-term stable supply hold irreplaceable advantages.

III. Core Advantages and Stable Production Capacity of Shanghai Lizhuo Pharmaceutical in Manufacturing 4-Bromo-3-fluoro-2-methylaniline

Shanghai Lizhuo Pharmaceutical has more than ten years of experience in fluoro-bromo substituted aromatic intermediates. 4-Bromo-3-fluoro-2-methylaniline is one of our regular mass-produced flagship products. Different from trading intermediaries, we own self-operated synthesis workshops, purification equipment and quality inspection labs, capable of undertaking lab trial samples, pilot batches and ton-level industrial orders simultaneously. Our core advantages fall into five categories:

1. Stable Mass Production Capacity Covering Orders of All Specifications

This product is continuously produced on dedicated production lines with supply capacity covering all procurement requirements:

  • · Trial sample specifications: 10g, 50g, 100g, 500g reagent grades for research institutions, free sample application supported;
  • · Pilot batches: Standard packages from 1kg to 50kg for small-scale trials and scale-up experiments of pharmaceutical factories;
  • · Large industrial batches: Annual framework supply agreements available for ton-level and above long-term orders to guarantee uninterrupted production of downstream factories. We own standardized synthesis workshops equipped with continuous low-temperature crystallization and purification equipment, free from raw material fluctuation impact with controllable delivery cycles. Domestic regular orders are shipped within 3–7 days, and foreign trade orders are supported with customs declaration and compliant hazardous chemical export procedures.

2. Strict Quality Control System with Stable Purity ≥97% and Zero Deviation in Parameters

All products leave the factory complying with unified corporate testing standards, with complete Certificate of Analysis (COA) attached to each batch:

1. HPLC testing of main content to steadily control purity above 97%, with strict control of fluoro/bromo substituted isomers and unreacted raw material impurities;

2. Special testing for density, boiling point, appearance and moisture, fully matching the physicochemical parameters published on the product detail page without false data labeling;

3. Finished products are vacuum-packed with aluminum foil under unified 2–8°C light-proof packaging to isolate light and air and avoid oxidation discoloration during transportation and storage;

4. Full batch retention and traceability system, with each batch retained for 12 months for rapid recheck and traceability upon customer quality complaints, complying with GMP audit requirements of pharmaceutical enterprises.

3. Independently Optimized Green Synthetic Process Delivering Dual Advantages in Cost and Quality

Our R&D team has iteratively upgraded the synthetic route of 4-Bromo-3-fluoro-2-methylaniline for years, delivering multiple strengths over traditional processes:

1. Low-temperature selective bromination and fluorination processes with fewer side reactions and low purification loss of crude products, resulting in higher product yield than the industry average;

2. Closed-loop solvent recovery system cutting production costs, offering highly competitive factory prices while maintaining high purity;

3. Green production process with low three-waste discharge and complete professional waste treatment equipment, holding full compliant production and pollutant discharge qualifications without production suspension due to environmental restrictions, ensuring stable supply in peak seasons.

4. Independent R&D Technical Support Providing Customized Deep Processing Services

The enterprise has an independent fine chemical R&D laboratory fully equipped with chromatography and mass spectrometry instruments, and the team boasts years of experience in synthesizing haloanilines:

1. We can provide technical consultation on processes and assist customers in optimizing downstream coupling and cyclization synthetic routes to lower R&D loss;

2. Customized higher purification grades available to meet stringent scenarios such as Class 1 new drug declaration;

3. One-stop procurement of supporting series fluoro-bromoanilines, organophosphine ligands and heterocyclic intermediates (e.g., 2-diphenylphosphinopyridine, (CAS 37943-90-1) to reduce customer costs of docking multiple suppliers.

5. Full-Range Supporting Services Connecting Domestic and Overseas Customers

1. Technical service: Provision of MSDS safety data sheets, COA test reports and product storage & operation guidelines, answering technical questions about storage, feeding and reaction processes;

2. Logistics and packaging: Special light-proof sealed chemical packaging for solid powder, delivered via low-temperature cold chain logistics to prevent deterioration under high temperature and light;

3. Multi-channel communication: Dedicated domestic and foreign sales teams reachable via email info@leichi-chem.com, charleen@leichi-chem.com and hotlines +86 139 6251 3054, +86 136 2174 3828 with 7×12-hour rapid response to inquiries, sample requests and orders;

4. After-sales guarantee: Free return, exchange and resupply of qualified batches if products fail appearance and purity standards upon arrival. Long-term cooperative customers enjoy preferential pricing and priority delivery policies.

IV. Procurement Summary

With its unique multi-substituted benzene ring structure containing fluorine, bromine, methyl and amino groups, 4-Bromo-3-fluoro-2-methylaniline (CAS 127408-03-1) serves as an irreplaceable high-end intermediate for new drug development, agrochemicals, organic synthesis and functional materials. Driven by the global growth of innovative pharmaceuticals and green chemical industries, the market demand for this product maintains steady long-term growth. However, products supplied by middlemen and small workshops on the market commonly suffer from insufficient purity, inconsistent batch performance and easy deterioration during storage, which will directly hinder the progress of downstream research and industrial production.

As a primary mass manufacturer of this product, Shanghai Lizhuo Pharmaceutical owns independent production lines and complete quality inspection equipment. Our products strictly comply with all physicochemical indicators displayed on the product detail page, featuring a stable purity of 97% and requiring standard light-shielded storage at 2–8°C. Our production capacity covers all order sizes ranging from lab samples to ton-level bulk shipments, delivering comprehensive advantages in production technology, product quality, pricing and supply stability. Whether you are a university laboratory, CRO research institute, API manufacturer or fine chemical plant, feel free to contact us for samples, quotations and complete technical documents if you need to purchase 4-Bromo-3-fluoro-2-methylaniline. We are ready to establish long-term and stable partnerships by providing premium products, competitive prices and all-round professional services.


Post time: Jun-23-2026