4‑Chloro‑5‑iodo‑7H‑pyrrolo[2,3‑d]pyrimidine (CAS: 123148‑78‑7) is a halogenated, N‑rich heterocyclic compound with the molecular formula C₆H₃ClIN₃ and a molecular weight of 279.47 g/mol. Its core structure — the pyrrolo[2,3‑d]pyrimidine bicycle, widely referred to as 7‑deazapurine — consists of a fused pyrrole and pyrimidine ring system that closely mimics the natural purine skeleton of ATP-binding protein kinase substrates. A chlorine atom at the 4‑position and an iodine atom at the 5‑position confer orthogonal reactivity: the 4‑position chlorine enables controlled nucleophilic aromatic substitution, while the 5‑position iodine opens the door to a wide range of cross‑coupling chemistries — a combination essential for exploring structure‑activity relationships (SAR) and for rapid, diversified functionalisation of the scaffold. As a direct structural analogue of the key heterocyclic cores found in clinically approved drugs, this compound occupies a critical position at the interface of medicinal chemistry and process development, making it one of the most sought‑after precursors for the next generation of targeted therapeutics.
Core Application Fields
Market demand for 4‑chloro‑5‑iodo‑7H‑pyrrolo[2,3‑d]pyrimidine is strongly concentrated in three major sectors: pharmaceutical intermediate for JAK inhibitors (≈65‑70% of total demand), kinase inhibitor library synthesis for oncology drug discovery (≈20‑25%), and nucleoside analogue development (≈5‑10%). The halogen‑functionalised 7‑deazapurine scaffold provides a versatile platform for a wide range of medically relevant targets.
1. JAK‑Inhibitor Synthesis (Dominant Application, 65‑70% of Demand). The vast majority of commercially produced 4‑chloro‑5‑iodo‑7H‑pyrrolo[2,3‑d]pyrimidine serves as an indispensable upstream building block in the multi‑step synthesis of several clinically approved Janus kinase (JAK) inhibitors. Pyrrolo[2,3‑d]pyrimidine derivatives lie at the heart of all currently marketed JAK inhibitors used for treating autoimmune diseases and myeloproliferative neoplasms. This intermediate has been explicitly employed in the synthesis of tofacitinib (Pfizer), as well as in the preparation of ruxolitinib (Incyte) and baricitinib — three blockbuster drugs that together account for annual sales exceeding USD 5‑8 billion. Ruxolitinib net product revenue alone totalled USD 764 million in Q2 2025 (+8% YoY) and contributed to Incyte‘s overall USD 1.15 billion quarterly sales.
The broader JAK inhibitor drug market shows strong growth across the board: it grew from USD 20.19 billion in 2024 to USD 23.76 billion in 2025 (CAGR 17.7 %). Other estimates place the global JAK inhibitor market at USD 20.7 billion in 2025, with projections pointing to a monumental USD 112 billion by 2034 (CAGR 20.6 %). Meanwhile, the narrower segment for JAK inhibitor drugs grew from USD 5.74 billion in 2024 to USD 6.42 billion in 2025 at 11.9 %. Autoimmune disorders drive this expansion: hospitalisations for rheumatoid arthritis in Australia increased 25 % year‑on‑year to 10,000 in 2021‑22. Psoriasis affects over 8 million people in the US and 125 million worldwide (2‑3 % of the global population). Diabetes was diagnosed in 28.7 million individuals (8.7 % of the US population), with 5.7 % requiring insulin. These figures underscore the urgent medical need that fuels JAK inhibitor demand — and consequently the demand for essential intermediates such as 4‑chloro‑5‑iodo‑7H‑pyrrolo[2,3‑d]pyrimidine.
2. Kinase‑Inhibitor Library for Oncology Discovery. The same 7‑deazapurine scaffold also serves as a privileged starting point for constructing diverse kinase inhibitor libraries aimed at cancer targets beyond JAK. The 4‑chloro‑5‑iodo substitution pattern has been used to synthesise functional analogues of Axl‑kinase inhibitors and also plays a role in the synthesis of nucleoside prodrugs for treating viral infections. The 5‑iodo group provides efficient access to Suzuki, Sonogashira and Buchwald‑Hartwig couplings for rapid SAR exploration, accelerating the discovery of novel anticancer compounds.
3. Nucleoside Analogue Development. As a 7‑deazapurine derivative, this intermediate is also applied in the synthesis of C‑nucleosides and related nucleoside analogues that possess antiviral and anticancer properties. In these applications it provides a purine‑like core that is resistant to glycosidic bond cleavage, thereby enhancing drug stability.
Major Market Participants
The global supply system for 4‑chloro‑5‑iodo‑7H‑pyrrolo[2,3‑d]pyrimidine (CAS 123148‑78‑7) follows a pattern of “specialized fine‑chemical and pharmaceutical‑intermediate manufacturers, primarily in China, Japan, India, and Europe, serving both small‑scale R&D and large‑scale production.” Key global manufacturers identified in industry reports include Nippon Fine Chemical (Japan), Angene International, BLDpharm, Combi‑Blocks, Hefei Xiuhe Biotech, Capot Chemical, and others. The compound is generally supplied as a white to off‑white crystalline solid with purity specifications of ≥98‑99 % (by HPLC) and a melting point in the range 179‑183 °C.
Shanghai XinChem Co., Ltd. (XinChem) has established a reliable, quality‑controlled supply chain for high‑purity 4‑chloro‑5‑iodo‑7H‑pyrrolo[2,3‑d]pyrimidine. Our product meets rigorous specifications: purity ≥98‑99 %, white to off‑white crystalline solid, controlled residual solvents, and low heavy metals — fully compliant with global pharmaceutical‑intermediate standards and suitable for both R&D (gram quantities) and industrial‑scale production (multi‑kg).
Regional Market Dynamics
Global demand for 4‑chloro‑5‑iodo‑7H‑pyrrolo[2,3‑d]pyrimidine 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, with Incyte, Pfizer, and AbbVie leading the market. 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 %) halogenated 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 — centres 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 4‑chloro‑5‑iodo‑7H‑pyrrolo[2,3‑d]pyrimidine at competitive prices. India’s rapidly growing generic JAK‑inhibitor sector — producing generic versions of tofacitinib, ruxolitinib and baricitinib — drives significant volume demand. Japan and South Korea demand ultra‑high‑purity grades for advanced API development. China’s market alone is expanding at a CAGR of 7‑9 %, fuelled by government biotech initiatives and expanding CRO/CDMO capacity. The compound is imported by Southeast Asian countries that are developing their own pharmaceutical manufacturing bases.
Market Size & Future Outlook
The market outlook for 4‑chloro‑5‑iodo‑7H‑pyrrolo[2,3‑d]pyrimidine is tied to the strong growth of the JAK‑inhibitor market. The global specialty intermediate market for this compound was valued at approximately US
1.0 – 2.0 millionin2024.Accordingtomarketresearchreports,theglobal4‑chloro‑5‑iodo‑7H‑pyrrolo[2,3‑d]pyrimidinemarketisexpectedtoreachUS 31 million by 2029, with a CAGR of 2.9 % during the forecast period (2023‑2029). The broader 7H‑pyrrolo[2,3‑d]pyrimidine intermediate market is experiencing rapid growth in both China and global markets, driven by the ongoing expansion of research on targeted cancer and autoimmune therapies.
Why Choose Shanghai XinChem Co., Ltd. (XinChem)
As a world‑leading supplier of organic chemicals and pharmaceutical intermediates, Shanghai XinChem Co., Ltd. (XinChem) has always focused on the innovative needs of the JAK‑inhibitor synthesis, oncology‑drug discovery and heterocyclic‑intermediate industries. Relying on core advantages in multi‑step heterocyclic synthesis, halogenation chemistry and rigorous quality assurance, we provide high‑purity 4‑chloro‑5‑iodo‑7H‑pyrrolo[2,3‑d]pyrimidine (CAS 123148‑78‑7) to global customers. Our product is manufactured under strict quality‑management systems, achieving consistent purity ≥98‑99 % (HPLC), a white to off‑white crystalline solid form, a melting point of 179‑183 °C, low residual solvents and ultra‑low heavy‑metal levels, fully complying with pharmaceutical‑intermediate standards. It is the ideal 7‑deazapurine building block for blockbuster JAK inhibitors, kinase‑inhibitor library synthesis, C‑nucleoside development and targeted drug discovery.
1. Technical Advantages
- High Purity & Consistency: Our product achieves ≥98‑99 % purity (by HPLC), white to off‑white crystalline solid, moisture <0.5 %, and a melting point of 179‑183 °C.
- 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 7‑Deazapurine Scaffold: Directly used in the synthesis of ruxolitinib, tofacitinib, baricitinib, and other pyrrolo[2,3‑d]pyrimidine‑based JAK inhibitors.
- Orthogonal Halogen Reactivity: The 4‑Cl site allows nucleophilic aromatic substitution for introducing side‑chain diversity; the 5‑I site provides a handle for cross‑coupling reactions (Suzuki, Sonogashira, Ullmann) during advanced intermediates and SAR library synthesis.
- Excellent Solvent Compatibility: Soluble in DMSO, ethyl acetate, methanol and common organic solvents used in pharmaceutical process development. It is partially soluble in water but has good solubility in typical heterocyclic synthesis solvents.
- Flexible Packaging: 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 fibre drums (industrial). Full custom packaging available for JAK‑inhibitor intermediates and heterocyclic building blocks.
- Reliable Supply Chain: Annual capacity 50‑200 kg, with dedicated temperature‑controlled warehousing (2‑8 °C, inert atmosphere recommended) and just‑in‑time delivery.
3. Application Fields
- Pharmaceutical intermediates: Key building block for JAK inhibitors (tofacitinib, ruxolitinib, baricitinib, upadacitinib) and next‑generation selective JAK/TYK2 inhibitors.
- Oncology drug discovery: Construction of diverse kinase‑inhibitor libraries (Axl, FAK, FLT3, BTK, EGFR) for targeted cancer therapy.
- Nucleoside analogue synthesis: Precursor for C‑nucleosides, antiviral agents and anticancer nucleoside drug candidates.
- Medicinal chemistry & SAR exploration: Halogenated scaffold enabling rapid diversification via cross‑coupling for hit‑to‑lead optimisation.
- Agrochemical R&D: Building block for developing heterocyclic crop‑protection agents.
4. Service Support
Our technical team provides impurity profiling (HPLC purity, residual solvents, heavy metals), custom synthesis of 7‑deazapurine derivatives, and regulatory documentation (Certificate of Analysis, Technical Data Sheet, Safety Data Sheet, REACH compliance, TSCA certification, DMF support for pharmaceutical customers). We offer cold‑chain logistics, custom packaging 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.
Contact us now to start cooperation!
Website: www.xinchem.com
Email: sales1@xinchem.com
WhatsApp: +86 18049800532
Post time: May-17-2026