2-Chloro-5-Bromobenzoic Acid Intermediate Dapagliflozin Synthesis Yield | NINGBO INNO PHARMCHEM
Role of BCBA in Hypoglycemic Drug Manufacturing
5-Bromo-2-chlorobenzoic acid (BCBA), identified by CAS 21739-92-4, serves as the foundational halogenated aromatic acid in the industrial synthesis of Dapagliflozin, a critical SGLT2 inhibitor for type 2 diabetes management. The structural integrity of the final API relies heavily on the precise positioning of the bromine and chlorine substituents on the benzoic acid ring. In standard organic synthesis routes, BCBA undergoes acyl chlorination followed by Friedel-Crafts acylation with 4-ethoxytoluene or phenetole derivatives to generate the key ketone intermediate. Any deviation in the regiochemistry or purity of the starting material directly compromises the stoichiometry and efficiency of these downstream transformations. Process chemists evaluating feedstock options must prioritize suppliers who guarantee consistent batch-to-batch performance to maintain stable reaction kinetics and minimize impurity carryover.
For a comprehensive technical breakdown of the manufacturing pathways, refer to our detailed documentation on 5-Bromo-2-Chlorobenzoic Acid Synthesis & Supply. This resource outlines the critical control points required to maintain high industrial purity levels throughout the production cycle.
Technical Specifications and Purity Grades for 5-Bromo-2-chlorobenzoic Acid Feedstock
NINGBO INNO PHARMCHEM CO.,LTD. manufactures BCBA to meet the rigorous demands of API producers. Our production capabilities support multiple purity grades, allowing procurement teams to select the optimal specification based on their specific synthesis route and cost-efficiency targets. We position our BCBA as a seamless drop-in replacement for legacy supplier codes, ensuring identical technical parameters while offering enhanced supply chain reliability and competitive bulk pricing. The chemical properties, including the melting point range of 154-156 °C, remain consistent across all grades, ensuring predictable handling and reaction behavior.
The following table outlines the comparative technical parameters for our standard and high-purity grades. Specific values for trace impurities and heavy metals should be verified against the batch-specific COA provided with each shipment.
| Parameter | Standard Grade | High Purity Grade | Test Method |
|---|---|---|---|
| Appearance | White to off-white powder | White powder | Visual Inspection |
| Melting Point | 154-156 °C | 154-156 °C | Capillary Method |
| Purity (HPLC) | ≥ 98.0% | ≥ 99.0% | HPLC |
| Loss on Drying | ≤ 0.5% | ≤ 0.3% | LOD |
| Residue on Ignition | ≤ 0.1% | ≤ 0.05% | ROI |
| Chloride Content | Please refer to the batch-specific COA | Please refer to the batch-specific COA | Titration |
Critical COA Parameters and ICH Q3 Compliance for Dapagliflozin Intermediates
When sourcing Bromochlorobenzoic acid for pharmaceutical applications, adherence to ICH Q3 guidelines regarding impurities is non-negotiable. The Certificate of Analysis (COA) must detail not only the main peak purity but also the profile of related substances, including potential isomers such as 2-bromo-5-chlorobenzoic acid and de-halogenated byproducts like 2-chlorobenzoic acid. These impurities can accumulate during the multi-step synthesis of Dapagliflozin, potentially triggering additional purification steps or failing final API specifications.
Field Engineering Insight: In pilot-scale acyl chlorination processes, our engineering team has observed that trace levels of 2-chlorobenzoic acid impurities (<0.1%) can disproportionately affect the color profile of the downstream ketone intermediate. While standard HPLC assays focus on the main peak, these trace impurities act as chromophore precursors during the subsequent Friedel-Crafts acylation, leading to yellowing in the final Dapagliflozin API. To mitigate this, we implement non-standard monitoring protocols that track specific isomeric impurities beyond the standard COA requirements. This proactive quality assurance approach ensures that the final API meets strict color specifications without requiring excessive decolorization carbon usage, thereby optimizing the overall manufacturing process efficiency.
Impact of BCBA Chromatographic Purity on Dapagliflozin Synthesis Yield
The chromatographic purity of the 5-Brom-2-chlor-benzoesaeure feedstock is directly correlated with the overall yield of the Dapagliflozin synthesis route. High-purity BCBA minimizes side reactions during the formation of the acyl chloride and the subsequent coupling with the ethoxy-aryl component. Impurities in the starting material often require stoichiometric excesses of reagents to drive the reaction to completion, increasing waste generation and downstream processing costs. By utilizing high-purity BCBA, process chemists can achieve tighter control over reaction endpoints and improve the mass balance of the synthesis.
NINGBO INNO PHARMCHEM CO.,LTD. provides a 5-bromo-2-chlorobenzoic acid high purity chemical intermediate that is engineered to maximize synthesis yield. Our product is designed to integrate seamlessly into existing manufacturing processes, offering a reliable alternative to established supplier codes without the need for process re-validation. This drop-in replacement strategy allows procurement teams to secure cost-efficient supply agreements while maintaining identical technical performance and quality standards.
Bulk Packaging Protocols and Nitrogen-Flushed Storage for Halogenated Benzoic Acids
Proper packaging and storage are essential to preserve the chemical integrity of halogenated benzoic acids during transit and warehousing. NINGBO INNO PHARMCHEM CO.,LTD. employs robust bulk packaging protocols to protect the product from moisture absorption and oxidation. Standard shipments are configured in 25kg multi-wall paper drums with inner polyethylene liners, suitable for most industrial applications. For larger volume requirements, we offer custom packaging options including Intermediate Bulk Containers (IBCs) to streamline handling and reduce material costs.
All drums are nitrogen-flushed prior to sealing to displace oxygen and minimize the risk of oxidative degradation during storage. This protocol is particularly critical for maintaining the stability of the product over extended periods or during transit through varying climatic conditions. Our logistics team coordinates shipping methods to ensure timely delivery while adhering to standard safety regulations for solid chemical intermediates. For specific packaging configurations or volume-based pricing, please contact our procurement specialists directly.
Frequently Asked Questions
What is the typical purity available for 5-Bromo-2-chlorobenzoic acid?
We offer BCBA in standard grades with purity ≥ 98.0% and high-purity grades with purity ≥ 99.0% as determined by HPLC. Exact purity values and impurity profiles are detailed in the batch-specific COA provided with each order.
Can your BCBA be used as a drop-in replacement for other supplier codes?
Yes. Our product is engineered to match the technical parameters of major competitor codes, ensuring seamless integration into existing synthesis routes. We focus on providing identical specifications with improved supply chain reliability and cost-efficiency.
What are the standard packaging options for bulk orders?
Standard packaging consists of 25kg multi-wall paper drums with inner liners, nitrogen-flushed for stability. We also provide custom packaging solutions, including IBCs, for large-scale procurement. Please refer to the batch-specific COA for detailed packaging specifications.
How does particle size affect the synthesis process?
Particle size distribution can influence dissolution rates and filtration efficiency during acyl chlorination. Our manufacturing process controls particle size to ensure consistent handling and reaction kinetics. Specific particle size data is available upon request and may be included in the COA.
What is the lead time for bulk supply?
Lead times vary based on order volume and current production schedules. We maintain strategic inventory levels to support rapid fulfillment. Contact our procurement team for accurate lead time estimates and to lock in supply agreements.
Sourcing and Technical Support
NINGBO INNO PHARMCHEM CO.,LTD. is committed to supporting R&D and manufacturing teams with high-quality 5-Bromo-2-chlorobenzoic acid intermediates. Our technical team is available to assist with specification reviews, COA analysis, and supply chain planning to ensure uninterrupted production of Dapagliflozin and related APIs. Partner with a verified manufacturer. Connect with our procurement specialists to lock in your supply agreements.