Industrial Manufacturing Process and Specifications for 3-Iodo-6-Nitro-1-(Tetrahydro-2H-Pyran-2-Yl)-1H-Indazole
- High Industrial Purity: Manufactured to >98% HPLC purity standards suitable for API synthesis.
- Scalable Synthesis Route: Optimized manufacturing process for kilogram to ton-scale production.
- Global Supply Chain: Reliable bulk price structures and documented quality assurance from NINGBO INNO PHARMCHEM CO.,LTD.
In the landscape of modern pharmaceutical intermediates, precision in chemical structure and consistency in batch quality are paramount. 3-Iodo-6-nitro-1-(tetrahydro-2H-pyran-2-yl)-1H-indazole serves as a critical building block in the synthesis of kinase inhibitors, particularly within the vascular endothelial growth factor (VEGF) receptor inhibitor class. As a global manufacturer, understanding the technical nuances of this compound is essential for procurement officers and process chemists alike. This document outlines the industrial specifications, manufacturing process capabilities, and quality control measures required for large-scale integration.
Overview of Heck Reaction Manufacturing Steps and Precursor Role
The production of complex indazole derivatives often begins with protected intermediates that ensure regioselectivity during subsequent coupling reactions. The manufacturing process for this specific nitro-indazole derivative involves careful control of protection groups, specifically the tetrahydropyran (THP) moiety, which safeguards the indazole nitrogen during harsh iodination and nitration conditions. While downstream derivatives may undergo Heck coupling to introduce vinyl-pyridine structures, the integrity of the initial iodo-nitro scaffold is the foundation of the entire synthesis route.
Industrial scale-up requires rigorous optimization of reaction parameters such as temperature control during diazonium formation or electrophilic substitution. Maintaining the stability of the nitro group while introducing the iodine atom demands specific catalytic conditions to minimize side products. Facilities operated by NINGBO INNO PHARMCHEM CO.,LTD. utilize advanced reactor systems to manage exothermic profiles, ensuring that the final product meets the stringent requirements for downstream API production. The ability to consistently produce this intermediate without significant degradation of the THP protecting group is a key marker of process maturity.
Technical Specifications and Physical Properties
For procurement teams evaluating suppliers, the physical and chemical properties dictate storage logistics and handling procedures. The following table summarizes the typical industrial specifications for this compound. These values are critical for establishing acceptance criteria in Quality Control (QC) laboratories.
| Parameter | Specification | Test Method |
|---|---|---|
| Chemical Name | 3-Iodo-6-nitro-1-(tetrahydro-2H-pyran-2-yl)-1H-indazole | - |
| CAS Number | 886230-74-6 | - |
| Molecular Formula | C12H12IN3O3 | - |
| Appearance | Light Yellow to Yellow Solid | Visual |
| Purity (HPLC) | >98.0% | Area Normalization |
| Melting Point | 145-155°C (Approx.) | DSC / Capillary |
| Storage Temperature | 2-8°C (Protect from Light) | - |
| Solubility | DMSO, Chloroform, Methanol | Experimental |
| Stability | Hygroscopic, Light Sensitive | Stability Study |
Attention to storage conditions is vital. Due to the presence of the nitro group and the iodine atom, the compound exhibits light sensitivity and hygroscopic tendencies. Improper storage can lead to hydrolysis of the THP group or decomposition of the nitro moiety, compromising the industrial purity required for subsequent steps. Therefore, all bulk shipments are packaged in light-resistant containers with appropriate desiccants to maintain integrity during transit.
Quality Control in Industrial Synthesis
Ensuring batch-to-batch consistency is the cornerstone of B2B chemical supply. Our quality assurance protocols involve multi-point verification throughout the production cycle. Every batch is accompanied by a comprehensive Certificate of Analysis (COA) that details impurity profiles, residual solvent levels, and heavy metal content. For process chemists validating a supply chain, the ability to trace impurities back to specific synthesis steps is invaluable.
When sourcing high-purity 3-Iodo-6-nitro-1-(oxan-2-yl)indazole, buyers should verify that the supplier employs High-Performance Liquid Chromatography (HPLC) and Nuclear Magnetic Resonance (NMR) spectroscopy for final release testing. The presence of de-protected indazole or over-iodinated byproducts must be kept below threshold limits to prevent catalysis poisoning in downstream coupling reactions. Advanced analytical methods allow for the detection of trace isomers that could affect the crystallization behavior of the final Active Pharmaceutical Ingredient (API).
Scalability for API Production and Bulk Procurement
The transition from laboratory scale to commercial production involves more than simply increasing reactor volume. It requires re-engineering the synthesis route to manage heat transfer, mixing efficiency, and filtration rates. Industrial manufacturing processes for indazole intermediates must account for the handling of hazardous reagents such as iodine sources and nitrating agents on a multi-kilogram scale.
Procurement strategies should focus on partners capable of delivering consistent bulk price advantages without sacrificing quality. Scale-up capabilities ensure that supply remains uninterrupted during clinical trial phases and commercial launch. NINGBO INNO PHARMCHEM CO.,LTD. maintains flexible production lines that can adapt to varying demand volumes, ensuring that project timelines are met without compromise. Whether requiring kilogram quantities for R&D or ton-scale supplies for commercialization, the infrastructure supports seamless scaling.
Safety and Handling Guidelines
Safety data indicates that this compound should be handled with standard precautions for nitro-aromatics and organic iodides. Personnel must utilize appropriate Personal Protective Equipment (PPE), including chemical-resistant gloves and safety eyewear. The material is classified with specific hazard statements regarding ingestion and skin irritation. Work should be conducted in a well-ventilated area or fume hood to minimize exposure to dust or vapors during weighing and transfer operations.
- Hazard Statements: Harmful if swallowed, causes skin irritation, causes serious eye irritation.
- Precautionary Statements: Wear protective gloves/protective clothing/eye protection/face protection.
- Disposal: Dispose of contents and container in accordance with local regulatory requirements.
In conclusion, the successful integration of 3-Iodo-6-nitro-1-(tetrahydro-2H-pyran-2-yl)-1H-indazole into a pharmaceutical supply chain relies on a partner with deep technical expertise and robust manufacturing capabilities. By prioritizing industrial purity, documented quality control, and scalable production, manufacturers can secure a reliable foundation for their API synthesis projects.