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The Quinoline Building Block That Lets Medicinal Chemists Separate Kinase Selectivity from Kinase Potency:4-Bromoquinolin-6-Amine (CAS 1260785-25-8)

4-Bromoquinolin-6-amine (CAS 1260785-25-8), also named 6-amino-4-bromoquinoline, is a bifunctional quinoline building block with the molecular formula C₉H₇BrN₂ and a molecular weight of 223.07. It presents as a solid and carries two handles on a single heteroaromatic core: a bromine atom at the 4-position and a primary aromatic amine at the 6-position. That substitution pattern is the molecule’s commercial rationale. The 4-bromo handle supports palladium-catalysed cross-coupling—Suzuki, Buchwald-Hartwig, Sonogashira and related transformations—while the 6-amino group provides a point for acylation, sulfonylation, alkylation or amide formation. A medicinal chemist can therefore elaborate the quinoline core in two independent directions without rebuilding the scaffold, which is why 4-bromoquinolin-6-amine is used in kinase inhibitor discovery and in the search for new antimalarial chemotypes. The compound appears explicitly in the aminoquinoline kinase inhibitor patent literature, including EP2680844, “AMINO-QUINOLINES AS KINASE INHIBITORS” , and it is catalogued by specialty suppliers as a building block for quinoline-based drug candidates targeting infectious disease and cancer. The market for this building block is not measured in tonnes. It is a research-to-pilot specialty chemical, supplied at ≥95% purity in 100 mg to 25 g packages, and its value is determined by the analytical confidence a supplier can provide: does the lot match the Certificate of Analysis, is the bromine intact, is the amine available for coupling, and can the material be documented for the buyer’s regulatory pathway. Published package pricing illustrates the scale: 100 mg at £48, 250 mg at £58, 1 g at £124, 5 g at £618 and 25 g at £2,593 from one UK-based supplier, with Chinese stock availability at the smaller sizes. The qualifying question for buyers is therefore not “what does a kilogram cost” but “which supplier can deliver a reproducible lot, with lot-specific analytical data, before the medicinal chemistry campaign loses time.”

Core Application Fields and Demand Architecture
Demand for 4-bromoquinolin-6-amine concentrates in three functional arenas where the 4-bromo-6-amino substitution pattern on the quinoline core is specifically useful: kinase inhibitor discovery, antimalarial and anti-infective research, and custom synthesis and scale-up services.

In kinase inhibitor discovery, the compound functions as a quinoline scaffold for ATP-competitive and allosteric inhibitors. The quinoline nitrogen and the 6-amino group can engage in hinge-region hydrogen bonding, while the 4-bromo position provides a vector for introducing aryl, heteroaryl or amino substituents through cross-coupling. The aminoquinoline scaffold is specifically disclosed in kinase inhibitor patent families, and the 4-bromo-6-amino pattern allows the medicinal chemist to vary the 4-substituent across a library while holding the 6-amino function constant, or vice versa. This is the segment where the building block’s value is highest, because the cost of a failed coupling or an off-spec lot is measured in lost synthesis time rather than in the price of the gram. A 95% lot that contains an unreported impurity or a partially reduced nitro precursor can produce a coupling product that requires chromatographic purification, and the medicinal chemist discovers the problem after the reaction rather than in incoming QC.

In antimalarial and anti-infective research, 4-aminoquinoline and related quinoline scaffolds have a long history in antiparasitic drug discovery, and 4-bromoquinolin-6-amine serves as a functionalized intermediate for introducing the 4-amino and 6-amino substitution patterns associated with antimalarial activity. The compound is also used in antimicrobial research, where quinoline derivatives are screened for activity against bacterial and fungal targets. This segment is smaller in volume than kinase discovery but is strategically important because it connects the building block to global health research funding streams that are less cyclical than commercial medicinal chemistry spending.

Custom synthesis and scale-up services form the third arena. Specialty suppliers offer 4-bromoquinolin-6-amine as a catalogue item and as a custom-synthesis starting point, and a program that begins with a 100 mg qualification lot may later require gram or tens-of-gram quantities under a locked specification. The suppliers visible in public listings include Fluorochem, ChemScene, CymitQuimica, SynQuest and a cohort of specialty producers, and the service dimension—the ability to follow a program from catalogue scale to custom scale without changing the analytical method or the impurity profile—is commercially important because the compound is rarely stocked in kilogram quantities.

Regulatory Profile: An R&D Building Block Defined by TSCA Non-Listing, Irritancy Classification and Analytical Identity
4-Bromoquinolin-6-amine is not a CMR substance in the pharmaceutical-excipient sense, and it is not classified as a dangerous good for transport. Its regulatory identity is defined instead by its inventory status, a handling-hazard classification, and the analytical specifications that determine whether the material is fit for medicinal chemistry.

The TSCA status is the single most consequential regulatory fact for U.S.-facing programs. SynQuest’s product record states explicitly that 4-bromoquinolin-6-amine is “Not listed on TSCA inventory”. For a substance not on the TSCA Inventory, manufacture or import into the United States for commercial purposes would ordinarily require a Premanufacture Notice or an applicable exemption, most commonly the R&D exemption under 40 CFR 720.36 for research and development quantities used by or directly under the supervision of a technically qualified individual. This means the compound’s U.S. commercial pathway is currently structured around research-scale supply, not commodity import, and buyers intending to use it in process development must confirm that their supplier’s TSCA position supports the intended use.

The hazard profile is that of a solid irritant rather than a CMR substance. The SDS reports GHS07 (Harmful/Irritant) with signal word “Warning” and hazard statements H302 (harmful if swallowed), H315 (causes skin irritation), H319 (causes serious eye irritation) and H335 (may cause respiratory irritation). These are handling hazards, not carcinogenicity, mutagenicity or reproductive toxicity classifications, and the compound is not reported as an SVHC. The required precautions are standard for a fine-chemical solid: avoid breathing dust, wear protective gloves and eye/face protection, use in a well-ventilated area, and store the container tightly closed. In the European Union, the compound falls outside the scope of REACH registration if manufactured or imported below one tonne per annum, and no SVHC listing applies. For Russian and EAEU buyers, the compound is imported at research and pilot scale, with documentation expectations centred on a Certificate of Analysis reporting identity and purity by HPLC and NMR, a Russian-language SDS, and confirmation that the material is the 4-bromo-6-amino isomer rather than a positional isomer or a partially reduced nitro precursor.

Global Supply Structure and Manufacturer Differentiation
Global supply of 4-bromoquinolin-6-amine is fragmented and research-oriented. The supplier landscape includes catalogue and research-chemical companies alongside specialty producers and custom-synthesis houses, with no single dominant manufacturer exercising capacity control. The suppliers visible in public listings span Fluorochem, ChemScene, CymitQuimica, SynQuest, Biozol, Indofine and a cohort of Chinese and other Asian producers, and the common specification is ≥95% purity with package sizes from 100 mg to 25 g. This fragmentation is typical of a building block at the pre-commercial stage: the molecule is made in batch quantities, often against projected demand or as part of a broader quinoline portfolio, and availability is measured in grams rather than in tonnes.

Differentiation operates on three axes. The first is analytical depth and lot-specific data. Suppliers that provide HPLC and NMR results for the specific lot, rather than a generic specification, reduce the buyer’s need to re-characterize material before use. In kinase discovery, where the building block is incorporated into a complex inhibitor and purification is expensive, the cost of an off-spec lot is measured in lost synthesis time rather than in the price of the gram. The second axis is isomeric and purity control. The 4-bromo-6-amino substitution pattern must be distinguished from positional isomers and from residual 4-bromo-6-nitroquinoline, the nitro precursor from which the amine is typically prepared by reduction. A lot that carries unreduced nitro precursor or a positional impurity will behave differently in cross-coupling and may introduce an impurity that is difficult to purge downstream. Suppliers that report the chromatographic purity and the absence of the nitro precursor give the medicinal chemist a defensible basis for use. The third axis is scale-up and custom-synthesis capability. A supplier that can follow a program from a 100 mg catalogue purchase to gram or tens-of-gram custom quantities, without changing the analytical method or the impurity profile, is more valuable than a catalogue vendor that cannot support the later stage.

Regional Demand Dynamics
Demand for 4-bromoquinolin-6-amine follows the geography of medicinal chemistry and biotech R&D rather than the geography of chemical manufacturing.

North America and Europe are the principal demand centres, reflecting the concentration of kinase inhibitor discovery, antimalarial and anti-infective research, and contract research organisations in these regions. Demand is project-driven and small in absolute mass: a single medicinal chemistry group may purchase 100 mg to a few grams at a time, and a program that advances may require tens of grams. The U.S. market carries the additional TSCA consideration described above, which tends to keep commercial flows at research scale unless an exemption or PMN pathway is established. European demand is similarly research-intensive, with buyers placing weight on supplier documentation and the ability to support custom synthesis as programs progress.

Asia-Pacific, and China in particular, is the manufacturing and stock-holding hub for the compound. Many catalogue suppliers maintain Chinese stock, and Chinese specialty producers offer the building block alongside custom-synthesis and scale-up services. The region’s demand is growing as domestic drug-discovery research expands, and Chinese suppliers are increasingly capable of providing ≥95% material with lot-specific analytical data. For Russian and EAEU buyers, China is the most accessible source of supply, with the practical qualification task centred on verifying the Certificate of Analysis and the SDS rather than on navigating a complex regulatory approval pathway.

Russia and the EAEU form a small, import-dependent contour. Demand comes from pharmaceutical R&D, medicinal chemistry groups and custom-synthesis service providers, and supply is sourced from Chinese and European catalogue vendors. There is no meaningful domestic production of the compound, and the practical constraint is availability at the required purity and package size rather than regulatory restriction. Buyers in the region place a premium on suppliers that can provide a Russian-language SDS, a lot-specific Certificate of Analysis and reliable delivery of small packages, because a delayed gram can stall a synthesis campaign.

Future Outlook and Strategic Imperatives
The commercial trajectory of 4-bromoquinolin-6-amine is tied less to its own market size than to the therapeutic areas it enables. Kinase inhibitor discovery remains one of the largest and most sustained areas of medicinal chemistry investment, and the aminoquinoline scaffold continues to appear in patent literature and in preclinical programs. Antimalarial and anti-infective research provides a second demand stream that is connected to global health funding and to the search for new chemotypes against resistant parasites. Custom synthesis adds a service layer that grows with every program that chooses the quinoline scaffold and needs a reproducible supply of the functionalized intermediate.

Three structural forces will shape the supply landscape. First, analytical transparency will remain the primary differentiator. As kinase programs mature, the building block’s purity and impurity profile directly affect the purity of the final inhibitor, and buyers will increasingly require lot-specific HPLC and NMR data, plus confirmation of the absence of the nitro precursor, rather than a nominal 95% figure. Second, the transition from catalogue to custom scale will separate suppliers that can support a program’s growth from those that can only fill a small-pack order. A supplier that can lock a specification at 100 mg and reproduce it at gram or tens-of-gram scale, with the same impurity profile, will be preferred for process development. Third, the TSCA non-listing will continue to shape U.S. market access. Suppliers that can clearly document the R&D-exempt basis for shipment, or that can support a PMN pathway for larger volumes, will be better positioned as U.S. programs advance beyond research scale.

For Russian and EAEU buyers, the strategic implication is that procurement should be treated as a specification-and-documentation decision rather than a price comparison. A nominal 95% lot that fails to meet the program’s purity requirement, or a shipment that arrives without a Russian-language SDS, can cost more in lost synthesis time than the price difference between two suppliers. The lowest-risk source is the one that can provide lot-specific analytical data, a clear statement of TSCA status for U.S.-linked programs, and the ability to scale the specification as the project advances.

Shanghai XinChem Co., Ltd. (XinChem)
As a world-leading supplier of organic chemicals, Shanghai XinChem Co., Ltd. (XinChem) offers 4-bromoquinolin-6-amine (CAS 1260785-25-8) in research-grade and custom-synthesis specifications, serving medicinal chemistry groups, kinase inhibitor discovery programs, antimalarial and anti-infective researchers, and pharmaceutical process development organisations. Our material is supplied with lot-specific analytical data, controlled isomeric purity and the documentation support that quinoline building-block qualification requires at both catalogue and scale-up stages.

Technical and Quality Advantages
Lot-Specific HPLC and NMR Data: 4-Bromoquinolin-6-amine is supplied with a Certificate of Analysis reporting identity and purity by HPLC and NMR for the specific lot, rather than a generic catalogue specification. For kinase and antimalarial programs, where the building block’s impurity profile affects downstream coupling and purification, lot-level data allows the buyer to qualify the material against the program’s actual requirements.

Isomeric Purity and Nitro-Precursor Control: The material is controlled for the 4-bromo-6-amino substitution pattern and for the absence of 4-bromo-6-nitroquinoline, the reduction precursor that can carry through into coupling reactions if the reduction is incomplete. This specification is more informative than a headline HPLC percentage, because a positional isomer or a nitro impurity can behave differently in cross-coupling and introduce a downstream impurity.

Purity at the ≥95% Threshold with Scale-Up Continuity: Material is available at ≥95% purity (HPLC), consistent with the research-grade specification used across the specialty supplier market, and can be supplied in custom-synthesis quantities under a locked specification. A program that begins with a 100 mg qualification lot can later scale without changing the analytical method or the impurity profile, reducing the re-qualification burden.

Regulatory and Documentation Support: Safety data sheets are available in English and Russian, with documentation covering the GHS07 irritant classification (H302, H315, H319, H335) and the current TSCA non-listing status. For U.S.-facing programs, XinChem provides clarity on the R&D-exempt basis for shipment, and for EAEU buyers the Russian-language SDS and Certificate of Analysis support incoming qualification.

Packaging and Logistics Flexibility
4-Bromoquinolin-6-amine is available in sealed 100 mg, 250 mg, 1 g and 5 g containers for research and medicinal chemistry use, and in larger package sizes for custom-synthesis and process-development quantities. For Russia and EAEU destinations, XinChem arranges logistics with appropriate customs and transport documentation, including Russian-language SDS and Certificate-of-Analysis support, to reduce clearance friction for a building block that is sourced internationally at research scale.

Application Support and Supply Reliability
XinChem’s technical team assists with grade selection for kinase inhibitor and antimalarial discovery, with cross-coupling and amide-formation strategy for the 4-bromo and 6-amino handles, and with the analytical and documentation requirements that quinoline building-block qualification demands. Supply schedules accommodate both catalogue-scale qualification orders and custom-synthesis volumes, with stock held for the package sizes most commonly requested in medicinal chemistry programs.

Why Choose XinChem
Expertise: Deep experience in quinoline and heteroaromatic building blocks, with application knowledge spanning kinase inhibitor discovery, antimalarial research and custom synthesis.
Consistency: Lot-specific control of identity, HPLC purity and isomeric composition—the parameters that determine whether the building block incorporates cleanly into a quinoline-based drug candidate or introduces a purification burden.
Compliance Readiness: Documentation structured around the GHS07 irritant classification, the current TSCA non-listing status and EAEU documentation expectations, with Russian-language SDS support.
Responsiveness: Direct technical and commercial access, with order structures from 100 mg qualification quantities to custom-synthesis volumes.

Contact us now to discuss your 4-bromoquinolin-6-amine requirements and request a specification sheet or qualification sample.
Website: www.xinchem.com
Email: sales1@xinchem.com
WhatsApp: +86 18049800532


Post time: Nov-01-2026