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5-Azaindole (1H-Pyrrolo[3,2-c]pyridine, CAS: 271-34-1) is a nitrogen-rich, fused bicyclic heterocycle with the molecular formula C₇H₆N₂ and a molecular weight of 118.14 g/mol [9†L7-L8]. Its unique structure — an indole bioisostere in which one of the aromatic ring carbons is replaced by a nitrogen atom — provides an additional hydrogen-bond acceptor site while preserving the planar geometry and π-rich electronic character of the indole system. This subtle “nitrogen-editing” approach confers superior metabolic stability, enhanced aqueous solubility, and favorable drug-like physicochemical properties to biologically active molecules built upon this foundation.

The growing utilization of azaindole derivatives as kinase inhibitors and their substantial contribution to drug discovery and innovation has solidified the scaffold‘s critical position at the interface of medicinal chemistry and pharmaceutical development [6†L11-L14][17†L7-L9]. In the adenosine triphosphate (ATP)-binding pocket of protein kinases, the two nitrogen atoms of the azaindole core participate in key hydrogen-bonding interactions, making it an exceptionally effective pharmacophore for achieving potent and selective kinase inhibition [17†L9-L14]. 5‑Azaindole is therefore widely recognized as one of the most valuable and most frequently deployed privileged heterocyclic templates in modern drug design. The core’s lone nitrogen substitution constitutes a highly refined “control knob” for tuning target binding affinity, improving metabolic resistance, and modulating overall pharmacokinetic performance [6†L23-L28].

Core Application Fields and Market Demand

Market demand for 5‑Azaindole is overwhelmingly concentrated in the pharmaceutical sector, where it serves as an indispensable upstream intermediate for the synthesis of several FDA-approved therapeutic agents and a vast number of drug candidates in active clinical development.

JAK and Bcr‑Abl Kinase Inhibitors (≈80–85% of total demand). 5‑Azaindole acts as a key synthetic precursor for various small‑molecule kinase inhibitors that target tyrosine kinases such as Janus kinases (JAK2/3) and Bcr‑Abl. JAK2 inhibitors built upon the azaindole scaffold have demonstrated high binding affinity and selectivity for the ATP-binding pocket of the JAK family, which plays a central role in cytokine and growth factor receptor signaling cascades [3†L14-L23][3†L25-L30]. This scaffold has been extensively investigated in both patent literature and high-impact medicinal chemistry publications for the treatment of myeloproliferative neoplasms and chronic myeloid leukemia (CML) [1†L4-L9][1†L15-L20]. The global JAK inhibitor market was valued at approximately USD 20.2 billion in 2024, grew to USD 23.8 billion in 2025 (CAGR 17.7 %), and is projected to reach USD 112 billion by 2034 (CAGR 20.6 %). The 5‑Azaindole intermediate market directly captures a share of this extraordinary growth.
FDA-Approved Drugs and Clinical‑Stage Kinase Inhibitors. Extensive compilations of FDA-approved drugs and clinical candidates bearing the azaindole core confirm the scaffold’s real-world drug discovery impact and its high regulatory acceptance for clinical development [4†L4-L7][15†L6-L7]. The scaffold has been investigated against a broad spectrum of oncology-relevant kinase targets, including adaptor-associated kinase 1 (AAK1), anaplastic lymphoma kinase (ALK), AXL, cell division cycle 7 (Cdc7), cyclin-dependent kinases (CDKs), fibroblast growth factor receptor 4 (FGFR4), phosphatidylinositol 3-kinase (PI3K), and proviral insertion site in moloney murine leukemia virus (PIM) kinases [17†L25-L36].
Coagulation Cascade Inhibitors. As a direct factor VIIa inhibitor, 5‑azaindole itself has demonstrated antithrombotic and anticoagulant activity, and its derivatives have been developed as inhibitors of both factor VIIa and thrombin, with utility for the treatment and prevention of thrombotic disorders [0†L11-L12][4†L28-L33].
Additional High-Value Pharmaceutical Applications. The scaffold has been used to prepare highly potent Cdc7 inhibitors with improved intrinsic metabolic stability; discovered as fluorinated CB2 PET radioligands for imaging neuroinflammation; incorporated into the first-in-class, orally bioavailable azaindole platform; and examined for activity against diverse biologically relevant targets including anthelmintic agents, angiotensin inhibitors, dopamine D4 ligands, and coagulation factors Xa/VIIa [1†L31-L35][4†L8-L14][5†L5-L6][5†L38-L43][6†L43-L47].
Material Science and Research Applications. Emerging applications in material science include use as a ligand for coordination chemistry, as a building block in the synthesis of advanced organic electronic materials (including OLEDs), and as a versatile scaffold for medicinal chemistry optimization and chemical probe development [3†L4-L9].

Synthetic Availability and Supply Chain Economics

The 5‑azaindole intermediate market is experiencing robust growth driven by the continuing expansion of kinase inhibitor pipelines worldwide. The compound is supplied as a white to off‑white crystalline powder with purity available from 97 % to ≥99 % by HPLC. Synthesis typically proceeds via multi‑step heterocyclic construction starting from pyridine-derived precursors. In China, annual production capacities reach the 100 kg to multi‑ton scale.

Pricing for 5‑azaindole generally follows a strong inverse-volume relationship. At R&D scale, 1 g of 98 % purity material retails for approximately USD 6–8 (RMB 48–58), while a 100 g bulk sample costs roughly USD 50–60 (RMB 400–4000) [2†L5-L6][10†L4-L7][11†L9-L11][12†L2-L3]. Kilogram-scale bulk quantities (≥1 kg) are available at substantial discounts via direct factory pricing.

Major Market Participants

The global supply system for 5‑azaindole follows a pattern of “specialized fine chemical and pharmaceutical intermediate manufacturers, primarily in China, India, Japan, Europe, and North America, serving both small‑scale R&D and large‑scale industrial production.”

Shanghai XinChem Co., Ltd. (XinChem) has established a reliable, fully quality‑controlled supply chain for high‑purity 5‑azaindole (CAS 271‑34‑1). Our product meets rigorous pharmaceutical intermediate specifications: purity ≥98–99 %, white to off‑white crystalline solid, controlled residual solvents, and strict heavy metal limits (≤10 ppm, ICH Q3D compliant). We maintain consistent batch‑to‑batch quality with full HPLC and NMR analytical release testing. XinChem is well‑positioned to serve the rapidly growing global demand from JAK inhibitor API manufacturers, CROs/CDMOs, and academic research institutions.

Regional Market Dynamics

Global demand for 5‑azaindole shows a distinct regional pattern: “North America and Europe lead in JAK inhibitor R&D and high‑purity pharmaceutical intermediate consumption, while Asia‑Pacific is the largest and fastest‑growing region for production and intermediate supply.”

North America (USA & Canada) accounts for the largest share of JAK inhibitor consumption. Robust NIH funding for oncology research, early‑stage drug discovery, and high demand for custom synthesis for clinical trials sustain North America‘s position as the biggest consumer of high‑purity (>99 %) heterocyclic intermediates. Many multinational pharmaceutical companies source their intermediates through CROs/CDMOs that strictly require full cGMP documentation.
Europe follows, led by Germany, Switzerland and the United Kingdom — centers of excellence in kinase inhibitor discovery. Regulations under REACH and EMA guidelines for API manufacturing force suppliers to provide comprehensive impurity profiling and full product traceability.
Asia‑Pacific is the most dynamic region. China has emerged as the dominant manufacturing hub for pharmaceutical heterocyclic intermediates, producing high‑purity 5‑azaindole at highly competitive prices. India‘s rapidly growing generic JAK inhibitor sector drives significant volume demand.

Regulatory and Environmental Considerations

5‑Azaindole (CAS 271‑34-1) is classified as an Xi irritant with potential for skin and eye irritation and may cause sensitization. The compound should be stored below 25 °C in a cool, dry, light‑protected environment, kept away from strong oxidizers and strong bases.

In the European Union, 5‑azaindole 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 use in the synthesis of pharmaceutical APIs, customers must adhere to cGMP guidelines (21 CFR Parts 210/211). In China, the compound is listed in the Inventory of Existing Chemical Substances (IECSC) and requires safety production licenses for manufacturing facilities.

Environmentally, 5‑azaindole has low aquatic toxicity and is moderately biodegradable. Manufacturing generates solvent‑containing waste streams and requires responsible disposal of organic by‑products. Green chemistry efforts focus on optimizing synthetic routes to improve yield, reduce the number of synthetic steps, and minimize waste generation.

Future Outlook

The market outlook for 5‑azaindole is tied to four powerful drivers: (1) the extraordinary growth of the JAK inhibitor market, projected to reach USD 112 billion by 2034 (CAGR 20.6 %); (2) the continuing expansion of targeted kinase inhibitor pipelines for oncology, autoimmune disorders, and inflammatory diseases; (3) the rapid growth of Asian CRO/CDMO sectors supplying intermediates to global pharmaceutical companies; and (4) the privileged status of 5‑azaindole as a“first‑choice” screening scaffold in fragment‑based drug discovery (FBDD) programs.

Challenges include: raw material availability for pyridine‑derived starting materials, the need for strict temperature‑controlled storage to prevent decomposition, and competition from alternative heterocyclic scaffolds (indole, 6‑azaindole, 7‑azaindole) for certain applications. Enterprises should focus on securing high‑purity (>99 %) 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, oncology drug discovery, and heterocyclic intermediate industries. Relying on core advantages in multi‑step heterocyclic synthesis, purification, and quality assurance, we provide high‑quality 5‑Azaindole (1H‑Pyrrolo[3,2‑c]pyridine, CAS 271‑34‑1) to global customers.

1. Technical Advantages

High Purity & Consistency: Our product achieves purity ≥98–99 % (HPLC), white to off‑white crystalline powder, molecular weight 118.14 g/mol, and moisture <0.5 % (KF titration).
Low Impurity Profile: Strict control of residual solvents, heavy metals (≤10 ppm, ICH Q3D compliant), and related substances ensures high synthetic performance.
Batch‑to‑Batch Uniformity: Rigorous analytical testing (HPLC, NMR) guarantees consistent quality, enabling reproducible yields in pharmaceutical production.

2. Product Advantages

Versatile JAK Inhibitor Scaffold: Directly used in the synthesis of JAK inhibitors, Bcr‑Abl inhibitors, and other kinase-targeted drug candidates.
Superior Pharmacophore for Drug Discovery: The 5‑azaindole core functions as an indole bioisostere with an additional hydrogen-bond acceptor atom, significantly improving solubility and metabolic stability over the parent indole system.
Flexible Packaging Options: 5 g, 10 g, 25 g, 50 g, 100 g, 500 g glass bottles (R&D); 1 kg HDPE containers (pilot); 5 kg, 10 kg, 25 kg fiber drums (industrial). Full custom packaging available.
Reliable Supply Chain: Annual capacity 100–500 kg, with dedicated temperature‑controlled warehousing (below 25 °C, cool dry storage) and just‑in‑time delivery.

3. Application Fields

Pharmaceutical Intermediates: Key building block for JAK inhibitors, Bcr‑Abl inhibitors, and next‑generation targeted cancer therapeutics.
Oncology Drug Discovery: Construction of diverse kinase inhibitor libraries for targeted cancer therapy (AAK1, ALK, AXL, Cdc7, CDKs, FGFR4, PI3K, PIM).
Anticoagulant Drug Development: Factor VIIa and thrombin inhibitors for thrombotic disorders.
Material Science: Ligand for coordination chemistry and building block for organic electronic materials (OLEDs).
Medicinal Chemistry & Chemical Probes: A first-choice scaffold for hit‑to‑lead optimization and fragment‑based drug discovery (FBDD).

4. Service Support
Our technical team provides full impurity profiling (HPLC purity, residual solvents, heavy metals by ICP‑MS), custom purification to any desired specification, and full 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 5‑azaindole 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, packaging sizes, and regulatory documentation requirements.
Cost‑effectiveness: High purity at competitive industrial pricing.

Post time: May-17-2026

The Privileged Heterocyclic Scaffold for JAK Inhibitors and Targeted Kinase Drug Discovery: 5-Azaindole (CAS 271-34-1)