6-Ethyl-5-Fluoropyrimidin-4-Ol Synthesis Route Industrial Purity and Bulk Supply
- Optimized Synthesis: Advanced manufacturing processes achieve yields exceeding 85% with minimal halogenated impurities.
- Commercial Grade Quality: Consistent batch-to-batch purity ≥99% suitable for scalable pharmaceutical production.
- Global Supply Chain: Reliable tonnage quantities with full regulatory documentation and factory-direct pricing.
In the landscape of modern antifungal pharmaceutical development, the efficiency of key starting materials dictates the commercial viability of the final active pharmaceutical ingredient (API). 6-Ethyl-5-fluoropyrimidin-4-ol serves as a critical Voriconazole intermediate, requiring precise control over reaction parameters to ensure optimal stereochemistry and impurity profiles. As demand for second-generation triazole antifungals grows, manufacturers must prioritize a robust synthesis route that balances high yield with stringent industrial purity standards.
At NINGBO INNO PHARMCHEM CO.,LTD., we specialize in the scale-up of complex heterocyclic building blocks. Our production facilities are engineered to overcome historical bottlenecks associated with pyrimidine functionalization, delivering material that meets the rigorous demands of process chemistry teams and procurement officers alike.
Technical Analysis: Synthesis Routes and Impurity Profiles
For R&D chemists and process engineers, the primary challenge in producing this pyrimidine derivative lies in the selective halogenation and subsequent hydrolysis steps. Legacy methods often relied on excessive phosphoryl chloride (POCl3), which proved difficult to remove completely, resulting in product purity levels below 80% and complicating downstream coupling reactions.
Modern manufacturing protocols have shifted towards milder conditions that enhance stereoselectivity and facilitate easier purification. Key technical considerations for scale-up include:
- Reaction Temperature Control: Maintaining strict thermal parameters (often between -15°C to 0°C during coupling phases) to minimize side reactions and racemization.
- Catalyst Selection: Utilizing optimized catalyst systems such as Pd/C or Raney nickel to ensure efficient dehalogenation without compromising the fluoro-substituent.
- Impurity Management: Effective removal of phosphorus residues and halogenated by-products is essential to prevent catalyst poisoning in subsequent Reformatsky-type coupling reactions.
By refining these parameters, contemporary processes can achieve overall yields of 85% to 90% with purity profiles exceeding 99%. This level of industrial purity is critical for ensuring the efficacy of the final antifungal agent and reducing the burden on downstream purification steps.
Quality Specifications and Technical Data
Consistency is the cornerstone of bulk chemical procurement. Our quality control laboratories utilize HPLC and GC-MS to verify every batch against strict internal standards. The following table outlines the typical technical specifications for our commercial grade material.
| Parameter | Specification | Test Method |
|---|---|---|
| Product Name | 4-Ethyl-5-Fluoro-6-Hydroxypyrimidine | - |
| CAS Number | 137234-87-8 | - |
| Molecular Formula | C6H7FN2O | - |
| Purity (HPLC) | ≥ 99.0% | Area Normalization |
| Related Substances | ≤ 0.5% (Total) | HPLC |
| Residual Solvents | Compliant with ICH Q3C | GC-Headspace |
| Heavy Metals | ≤ 10 ppm | ICP-MS |
| Appearance | White to Off-White Solid | Visual |
When sourcing high-purity 4-Ethyl-5-Fluoro-6-Hydroxypyrimidine, buyers should verify that the supplier provides batch-specific data regarding residual halogens and phosphorus content, as these are common failure points in audit scenarios.
Procurement Strategy and Supply Chain Stability
For procurement managers and executive decision-makers, securing a reliable supply chain is as vital as the chemical specifications themselves. Market volatility can impact bulk price stability, particularly for fluorinated heterocycles where raw material costs fluctuate. Partnering with a dedicated global manufacturer mitigates these risks through vertical integration and long-term inventory planning.
Our facility offers distinct advantages for large-scale contracts:
- Scalable Production: Capacity to supply tonnage quantities to support commercial API manufacturing without lead time delays.
- Regulatory Compliance: Documentation support including REACH, TSCA, and DMF availability to streamline your regulatory filings.
- Custom Synthesis: Flexibility to adjust particle size or packaging requirements based on your specific process needs.
Transparency in documentation is non-negotiable. We ensure that every shipment is accompanied by a comprehensive COA (Certificate of Analysis) and Safety Data Sheet (SDS). This commitment to documentation facilitates faster quality assurance release times upon receipt at your facility.
Conclusion
The production of high-performance antifungal agents relies heavily on the quality of the heterocyclic building block supply chain. By leveraging advanced pharmaceutical synthesis techniques and maintaining strict quality controls, NINGBO INNO PHARMCHEM CO.,LTD. ensures that our clients receive material that drives efficiency in their own production lines.
To discuss your specific requirements for this intermediate, please contact our technical sales team for a batch-specific COA, SDS, or bulk pricing quote. We are ready to support your development timelines with reliable supply and expert technical consultation.