Industrial Purity and COA Specifications for 4-Benzyl-2-Hydroxy-Morpholin-3-One
- High Purity Standards: Industrial grade material typically exceeds 98.0% purity via GC analysis.
- Critical Application: Serves as a key Fosaprepitant intermediate in NK1 receptor antagonist synthesis.
- Bulk Availability: Scalable manufacturing processes ensure consistent supply for pharmaceutical production.
In the pharmaceutical manufacturing sector, the reliability of chemical intermediates directly impacts the quality of the final active pharmaceutical ingredient (API). 4-Benzyl-2-hydroxy-morpholin-3-one, identified by CAS number 287930-73-8, is a critical morpholinone derivative utilized extensively in the production of antiemetic drugs. As a global manufacturer committed to quality, NINGBO INNO PHARMCHEM CO.,LTD. ensures that every batch meets rigorous analytical standards required for GMP environments. This compound, with the molecular formula C11H13NO3, requires precise handling and verification to maintain industrial purity levels suitable for downstream synthesis.
Physical and Chemical Property Specifications
Understanding the physicochemical properties of this intermediate is essential for process chemists during scale-up production. The material typically presents as a white to off-white crystalline solid. Accurate characterization ensures that the material behaves predictably during reaction conditions. Below is a standard specification table reflecting typical industrial data points found on a Certificate of Analysis.
| Property | Specification |
|---|---|
| CAS Number | 287930-73-8 |
| Molecular Formula | C11H13NO3 |
| Molecular Weight | 207.23 g/mol |
| Melting Point | 134.0 °C to 138.0 °C |
| Appearance | White to Off-White Solid |
| Purity (GC/HPLC) | > 98.0% |
| Density | 1.292 ± 0.06 g/cm³ (Predicted) |
| Storage Conditions | Sealed in dry, Room Temperature |
Synthesis Route and Manufacturing Process
The synthesis route for this compound generally involves the condensation of N-benzylethanolamine with glyoxalate. In an optimized manufacturing process, a 50% aqueous solution of glyoxalate is reacted with N-benzylethanolamine in a solvent system such as tetrahydrofuran under reflux conditions. Following the reaction, the solvent is removed, and the residue is treated with water to promote crystallization. This method typically affords the target product with a yield exceeding 90%.
For buyers evaluating suppliers, understanding the benzyl lactam lactol structure is vital. Impurities often arise from incomplete cyclization or over-oxidation. Therefore, robust purification steps, including recrystallization from ice water, are necessary to remove residual starting materials. When sourcing high-purity 4-Benzyl-2-hydroxymorpholin-3-one, buyers should verify that the supplier employs strict control over reaction temperature and pH to minimize side products.
HPLC and NMR Testing Protocols for Verification
Quality assurance relies on advanced analytical techniques. A comprehensive COA should include data from both High-Performance Liquid Chromatography (HPLC) and Nuclear Magnetic Resonance (NMR) spectroscopy. HPLC is used to quantify the main peak area, ensuring it meets the >98.0% threshold. Any related substances or degradation products must be identified and quantified below acceptable limits.
NMR spectroscopy provides structural confirmation. Proton NMR spectra should display characteristic signals for the benzyl protons and the morpholinone ring protons. The presence of specific chemical shifts confirms the correct regiochemistry of the hydroxyl group at the 2-position. Batch consistency is maintained by comparing these spectral fingerprints against a reference standard. This level of detail distinguishes factory direct suppliers capable of supporting complex pharmaceutical pipelines from general trading companies.
Understanding Certificate of Analysis Data Points
The Certificate of Analysis is the primary document for quality verification. Key data points include the batch number, manufacturing date, and expiration date. Safety data is also critical; the material typically carries a GHS07 symbol with hazard statements H315 and H319, indicating potential skin and eye irritation. Precautionary statements such as P264 and P280 should be followed during handling.
Furthermore, the MSDS provides essential information regarding transport and storage. The compound is stable under recommended conditions but should be protected from moisture to prevent hydrolysis. For large-scale operations, the HS Code 2934.99.4400 is commonly used for customs clearance. Ensuring that the COA aligns with these regulatory codes prevents delays in international shipping.
Batch Consistency Standards for Pharmaceutical Intermediates
Consistency across batches is paramount for API synthesis. Variations in particle size or moisture content can affect reaction kinetics in subsequent steps. Leading manufacturers implement Statistical Process Control (SPC) to monitor critical quality attributes. This ensures that the bulk price reflects not just the quantity, but the reliability of the supply chain.
NINGBO INNO PHARMCHEM CO.,LTD. maintains rigorous batch consistency standards to support clients in the production of Fosaprepitant and related compounds. By controlling the crystallization process and drying parameters, the company ensures that physical properties remain within tight tolerances. This reliability reduces the risk of batch failure during the final drug substance manufacturing.
Commercial Availability and Bulk Procurement
Market analysis indicates significant price variations between gram-scale research quantities and multi-kilogram industrial orders. While small packs may command higher unit costs, scale-up production capabilities allow for competitive bulk price structures. Procurement teams should request quotes based on annual consumption volumes to secure optimal terms.
Packaging options typically range from 1 kg foil bags to 25 kg drums, depending on the customer's needs. Proper packaging ensures the material remains stable during transit. For projects requiring custom synthesis or specific particle size distributions, direct communication with the manufacturing team is recommended. This collaborative approach ensures that the intermediate meets the specific process requirements of the downstream synthesis.
Conclusion
4-Benzyl-2-hydroxy-morpholin-3-one is a vital component in the synthesis of modern antiemetic therapies. Ensuring high industrial purity through rigorous testing and reliable manufacturing processes is essential for pharmaceutical success. By partnering with a dedicated manufacturer like NINGBO INNO PHARMCHEM CO.,LTD., companies can secure a stable supply of this critical Fosaprepitant intermediate. Prioritizing technical specifications and batch consistency ultimately safeguards the quality of the final medicinal product.