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Pyrrolo[2,3-c]pyridine-3-ylamine dihydrochloride (also known as 3-Amino-6-azaindole dihydrochloride, CAS 1257535-55-9) is a nitrogen-rich bicyclic heterocycle with the molecular formula C₇H₉Cl₂N₃ and a molecular weight of 206.07 g/mol. Its core structure — the azaindole ring system — is a bioisostere of the natural indole backbone, with a strategically placed nitrogen atom that provides an additional hydrogen bond acceptor site while preserving the planar geometry and π-rich electronic character essential for high-affinity ATP-competitive binding to kinase active sites. The dihydrochloride salt form ensures excellent stability, water solubility, and compatibility with standard peptide synthesis workflows, making it the ideal shelf-stable building block for early-stage medicinal chemistry campaigns.

Azaindole derivatives have emerged as one of the most privileged and most extensively deployed scaffolds in modern kinase inhibitor drug discovery, with a rapidly expanding library of FDA-approved and clinical-stage therapeutics built upon this core. The scaffold‘s unique ability to participate in multiple hydrogen-bonding interactions within the ATP-binding hinge region of protein kinases gives it an exceptionally versatile and high-performance pharmacophore profile. Pyrrolo[2,3-c]pyridine-3-ylamine dihydrochloride has therefore become the indispensable synthetic precursor for countless pharmaceutical discovery programs aimed at highly validated oncology and autoimmune targets.

Core Application Fields and Market Demand

JAK Inhibitor Development — The pyrrolopyridine scaffold has demonstrated significant inhibitory activity on JAK family proteins (JAK1, JAK2, JAK3, and TYK2) and is recognized as a highly effective structural platform for developing novel JAK-targeted therapeutics. JAK inhibitors built upon the azaindole scaffold have successfully yielded several FDA-approved drugs for the treatment of rheumatoid arthritis, psoriatic arthritis, ulcerative colitis, alopecia areata, and myelofibrosis. The JAK-STAT pathway is intricately governed by over 50 signal molecules binding to approximately 40 receptor pairs, making JAK inhibition one of the most intensively pursued strategies for managing autoimmune disorders and hematological malignancies. 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 an extraordinary USD 112 billion by 2034 (CAGR 20.6%), reflecting a sustained and powerful demand surge. This compounds’ core scaffold is positioned to directly capture a significant share of this dramatic growth.

Kinase Inhibitor Library Synthesis — The compact azaindole core serves as the ideal hinge-binding motif for generating diverse kinase inhibitor libraries. Researchers have employed this scaffold to develop potent and selective inhibitors targeting a broad range of clinically relevant kinases beyond JAK, including Cdc7, AAK1, ALK, AXL, FAK, FGFR4, PI3K, and PIM kinases. The 3-amino functional group provides an accessible vector for rapid, efficient diversification via standard amide coupling, Buchwald-Hartwig amination, and nucleophilic aromatic substitution chemistries. Notably, current research has reported C-5 substituted pyrrolopyridine derivatives that display 352‑/253‑fold selectivity for JAK1 over JAK2 in enzyme assays, marking a 10‑fold improvement in both potency and selectivity over previous lead compounds — underscoring the scaffold‘s exceptional potential for generating high-quality clinical candidates. The global kinase inhibitor market was valued at USD 59.4 billion in 2024 and is projected to reach USD 79.9 billion by 2031 (CAGR 4.4%), with other reports estimating an even more aggressive trajectory from USD 57.2 billion in 2025 to USD 113.2 billion by 2034 (CAGR 7.9%). Pyrrolo[2,3-c]pyridine-3-ylamine dihydrochloride occupies the critical position at the beginning of this multi‑billion dollar value chain.

Drug Discovery Hit-to-Lead Optimization — As a direct structural analog of the core heterocycles found in clinically approved kinase inhibitors, this compound serves as a first-choice screening scaffold in fragment‑based drug discovery (FBDD) programs. The 3‑amino group and the two chloride counter‑ions, the compound provides a bench‑stable, easily handleable, and readily characterizable starting point for medicinal chemists to rapidly explore structure‑activity relationships (SAR) through parallel synthesis workflows.

Antiviral and Anticancer Research — Studies have demonstrated that derivatives of 3‑amino‑6‑azaindole can inhibit specific viral replication pathways and exhibit cytotoxic effects against cancer cell lines, further broadening the scaffold‘s therapeutic potential. The compound‘s primary mechanism of action — inhibition of protein kinases — can lead to significant changes in the growth, proliferation, differentiation, migration, and apoptosis of tumor cells, potentially suppressing tumor growth and progression. These properties make pyrrolo[2,3-c]pyridine-3-ylamine dihydrochloride an invaluable starting point for exploring a wide array of antiviral and oncology drug development pipelines.

Major Market Participants

The global supply system for pyrrolo[2,3-c]pyridine-3-ylamine dihydrochloride 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.” The compound is generally supplied as a white to off-white crystalline powder with purity ranging from 95% to ≥99% by HPLC. Market prices reflect R&D-grade material with transparent inverse‑volume pricing: bulk 1g and 5g quantities from specialized suppliers are sold at competitive wholesale rates, with the premium reflecting the synthetic complexity and the essential value of this cornerstone heterocycle.

Shanghai XinChem Co., Ltd. (XinChem) has established a reliable, fully quality‑controlled supply chain for high‑purity pyrrolo[2,3-c]pyridine-3-ylamine dihydrochloride (CAS 1257535-55-9). Our product meets rigorous pharmaceutical intermediate specifications — purity ≥98‑99% (HPLC), white to off-white crystalline powder, controlled residual solvents (<0.5% total), strict heavy metals (Pb, As, Cd, Hg ≤10 ppm, ICH Q3D compliant), and moisture <0.5% (KF titration) — fully compliant with global kinase inhibitor and oncology drug discovery standards. 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 pyrrolo[2,3-c]pyridine-3-ylamine dihydrochloride is segmented into three distinct patterns: North America and Europe lead in JAK inhibitor R&D and high‑purity pharmaceutical intermediate consumption; Asia‑Pacific is the largest and fastest‑growing region for production and intermediate supply; and Latin America and Middle East/Africa are emerging growth regions with increasing CRO/CDMO activity.

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%) azaindole scaffolds. 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 azaindole intermediates, producing high‑purity pyrrolo[2,3-c]pyridine-3-ylamine dihydrochloride at highly competitive prices. India’s rapidly growing generic JAK inhibitor sector drives significant volume demand. Japan and South Korea demand ultra‑high‑purity grades for advanced API development. The Chinese market alone is expanding at a CAGR of 7‑9%, fueled by government biotech initiatives and rapidly expanding CRO/CDMO capacity.

Regulatory and Environmental Considerations

Pyrrolo[2,3-c]pyridine-3-ylamine dihydrochloride (CAS 1257535-55-9) is classified as an Xi irritant with potential for skin and eye irritation. It may cause skin and respiratory tract sensitization. The compound should be stored below 25 °C in a cool, dry, light‑protected environment, kept away from strong oxidizers and strong bases, and the free base amine should be protected from prolonged exposure to air. The dihydrochloride salt form provides enhanced stability during handling and long‑term storage compared to the free base amine.

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 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, the compound 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 pyrrolo[2,3-c]pyridine-3-ylamine dihydrochloride 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 the azaindole scaffold as a “first‑choice” screening platform 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 azaindole isomers (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 anti‑inflammatory API industries. Relying on core advantages in multi‑step heterocyclic synthesis, purification, and quality assurance, we provide high‑quality Pyrrolo[2,3-c]pyridine-3-ylamine dihydrochloride (3‑Amino‑6‑azaindole dihydrochloride, CAS 1257535-55-9) to global customers.

1. Technical Advantages

High Purity & Consistency: Our product achieves purity ≥98‑99% (HPLC), white to off-white crystalline powder, molecular weight 206.07 g/mol, melting point >300°C (decomposition), and moisture <0.5% (KF titration).
Low Impurity Profile: Strict control of residual solvents, heavy metals (≤10 ppm, ICH Q3D compliant), and related substances by HPLC‑UV ensures high synthetic performance and batch‑to‑batch reproducibility.
Dihydrochloride Salt Stability: The dihydrochloride formulation provides exceptional shelf stability (≥24 months) when stored properly, significantly outperforming the free base amine for long‑term archiving of reference standards.
Batch‑to‑Batch Uniformity: Rigorous analytical testing (HPLC, NMR, LC‑MS, heavy metals by ICP‑MS, residual solvents by GC‑headspace) guarantees consistent quality, enabling reproducible yields in pharmaceutical production.

2. Product Advantages

Versatile Azaindole Scaffold: Directly used in the synthesis of JAK inhibitors (JAK1‑selective, JAK2‑targeting), next‑generation kinase‑targeted drug candidates, and azaindole-based library generation.
Superior Pharmacophore for Kinase Inhibition: The 6‑azaindole core functions as an ideal hinge‑binding motif with an additional hydrogen bond acceptor, providing improved binding affinity and selectivity over the parent indole system.
Bench‑Stable Dihydrochloride Form: Supplied as a stable, non‑hygroscopic (when properly sealed), easy‑to‑weigh crystalline solid — safe for routine laboratory handling without specialized inert atmosphere glove boxes.
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 for pharmaceutical campaigns.
Reliable Supply Chain: Annual capacity 100‑500 kg, with dedicated temperature‑controlled warehousing (below 25 °C, inert atmosphere recommended for long-term storage) and just‑in‑time delivery capabilities.

3. Application Fields

Pharmaceutical Intermediates: Key building block for JAK inhibitors (JAK1, JAK2, TYK2), next‑generation targeted cancer therapeutics, and kinase‑directed drug discovery.
Oncology Drug Discovery: Construction of diverse azaindole-based kinase inhibitor libraries for targeted cancer therapy (Cdc7, AAK1, ALK, AXL, FAK, FGFR4, PI3K, PIM, BTK, FLT3).
Autoimmune Disease APIs: Intermediate for drug candidates targeting rheumatoid arthritis, psoriasis, ulcerative colitis, alopecia areata, inflammatory bowel disease, and Crohn‘s disease.
Medicinal Chemistry & SAR Exploration: A first‑choice scaffold for hit‑to‑lead optimization, fragment‑based drug discovery (FBDD), and structure‑activity relationship campaigns.
Antiviral and Antimicrobial Research: Building block for exploring viral replication inhibition and cytotoxic effects against cancer cell lines.

4. Service Support
Our technical team provides full impurity profiling (HPLC purity, 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 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 Essential Azaindole Scaffold for JAK Inhibitors and Targeted Drug Discovery: Pyrrolo[2,3-c]pyridine-3-ylamine dihydrochloride (CAS 1257535-55-9)