6-Azido-2-Fluoropurine Synthesis Route & Bulk Scaling Guide
Procurement teams and R&D directors face significant challenges in securing stable supplies of critical fluorinated purine derivatives. Traditional synthesis methods often suffer from low yields during late-stage fluorination, leading to wasted costly chlorosugar intermediates and inconsistent industrial purity. Scaling these processes requires a convergent synthesis route that introduces the fluoro group early to maximize efficiency and reduce overall manufacturing costs.
Detailed Chemical Synthesis Route and Reaction Mechanism
The optimized synthesis route for 6-Azido-2-Fluoropurine begins with the azidation of 2-amino-6-chloropurine. This starting material is heated with an alkali metal azide, preferably sodium azide (NaN3), in a polar solvent such as aqueous dimethyl sulfoxide (DMSO). Reaction temperatures are maintained between 100°C and 110°C for 12 to 24 hours to yield 2-amino-6-azidopurine. This step ensures high conversion before the critical fluorination occurs.
Subsequently, the intermediate undergoes diazotization and fluorination. The reaction medium typically comprises a diazotization agent like t-butylnitrite and a fluorination agent such as aqueous fluoboric acid (HBF4) in tetrahydrofuran (THF). The process initiates below 0°C and warms to ambient temperature, completing within 3 hours. This convergent approach allows the production of a high-quality nucleoside intermediate suitable for coupling with protected chlorosugars. By introducing the 2-fluoro group before the coupling step, manufacturers significantly reduce the amount of expensive sugar derivatives required, improving the overall economic viability of fludarabine production.
Technical Specifications and Analytical Methods
Ensuring industrial purity is paramount for downstream pharmaceutical applications. Our manufacturing process adheres to strict quality control protocols, utilizing advanced spectroscopic techniques for characterization. The compound may exist in equilibrium with its tetrazolo-tautomer, but this does not detract from its utility as a synthetic building block. Below are the standard specifications provided with every Certificate of Analysis (COA).
| Parameter | Specification |
|---|---|
| Product Name | 6-Azido-2-Fluoro-7H-Purine |
| CAS Number | 143482-58-0 |
| Molecular Formula | C5H2FN7 |
| Purity (HPLC) | >98.5% |
| Appearance | Off-white to Pale Yellow Solid |
| Analysis Methods | 1H NMR, 13C NMR, MS, HPLC |
| Packing | 25kg Drum or Custom IBC |
Industrial Packaging Options and Global Logistics
As a reliable global manufacturer, we understand that secure logistics are as critical as chemical quality. 6-Azido-2-Fluoropurine is packaged in sealed drums or Intermediate Bulk Containers (IBCs) to prevent moisture ingress and degradation during transit. We handle all hazardous material documentation required for international shipping, ensuring compliance with IMDG and IATA regulations. For procurement officers evaluating long-term contracts, understanding market trends is essential. You can review the latest 6-Azido-2-Fluoropurine Bulk Price Quote 2026 to align your budgeting with current production capacities and raw material costs.
NINGBO INNO PHARMCHEM CO.,LTD. is committed to providing stable supply chains for complex Azido Purine Derivatives. We support custom synthesis requests and offer volume-based pricing structures to meet the demands of large-scale pharmaceutical production. Partner with a verified manufacturer. Connect with our procurement specialists to lock in your supply agreements.