Strategic Importance of Acetyl Dapagliflozin CAS 461432-25-7 in Pharmaceutical Synthesis

In the intricate landscape of pharmaceutical manufacturing, high-purity intermediates are paramount for the efficient and cost-effective production of Active Pharmaceutical Ingredients (APIs). Acetyl Dapagliflozin CAS 461432-25-7 stands as a critical advanced intermediate in the synthesis of Dapagliflozin, a widely recognized SGLT2 inhibitor. This compound's precise molecular structure and reactivity make it indispensable in the multi-step synthetic pathways required to produce pharmaceutical-grade Dapagliflozin, which is extensively used in the management of type 2 diabetes mellitus, heart failure, and chronic kidney disease.

Understanding the comprehensive profile of Acetyl Dapagliflozin CAS 461432-25-7 – from its technical specifications and manufacturing process to its strategic application advantages and market dynamics – is crucial for B2B stakeholders, including pharmaceutical manufacturers, contract research organizations (CROs), and specialty chemical suppliers. This article delves into these aspects, providing a detailed overview tailored for technical decision-makers and procurement specialists.

Industry Trends and Market Dynamics for SGLT2 Inhibitors

The global market for SGLT2 inhibitors has witnessed robust growth over the past decade, driven by increasing prevalence of diabetes, expanding indications for these drugs (including cardiovascular and renal benefits), and growing awareness among healthcare providers. This expansion directly fuels the demand for key intermediates like Acetyl Dapagliflozin CAS 461432-25-7. Market research reports project the global SGLT2 inhibitor market to reach over $30 billion by 2027, with a Compound Annual Growth Rate (CAGR) exceeding 10%.

Key trends impacting the demand for this intermediate include:

• Rising Global Diabetes Incidence: The International Diabetes Federation (IDF) estimates that 537 million adults globally are living with diabetes, a number projected to rise significantly, sustaining the demand for effective treatments.
• Expanded Therapeutic Indications: Beyond type 2 diabetes, SGLT2 inhibitors like Dapagliflozin are now approved for heart failure with reduced ejection fraction and chronic kidney disease, broadening their market reach.
• Focus on Cost-Efficiency: Pharmaceutical companies are continuously seeking more efficient and cost-effective synthetic routes and reliable suppliers for intermediates to manage production costs and enhance market competitiveness.
• Supply Chain Resilience: Geopolitical events and global health crises have underscored the importance of diversified and resilient supply chains for critical pharmaceutical raw materials and intermediates.

Manufacturers capable of supplying high-purity Acetyl Dapagliflozin CAS 461432-25-7 consistently and reliably are therefore positioned to capitalize on this expanding market. The emphasis on quality, regulatory compliance, and robust supply chain management is more critical than ever.

Technical Specifications of Acetyl Dapagliflozin CAS 461432-25-7

As a critical intermediate, the purity and precise characterization of Acetyl Dapagliflozin CAS 461432-25-7 are paramount. Deviations can significantly impact the final API's yield, purity, and regulatory acceptance. Key technical parameters are rigorously controlled and analyzed using advanced chromatographic and spectroscopic techniques.

General Product Information

• Product Name: Acetyl Dapagliflozin
• CAS Number: 461432-25-7
• Molecular Formula: C₂₅H₂₉ClO₇
• Molecular Weight: 477.95 g/mol
• Appearance: White to off-white crystalline powder
• Storage Conditions: Store in a cool, dark, and dry place, preferably under inert atmosphere.

Key Analytical Parameters (Example Specification Sheet)

These stringent specifications ensure that Acetyl Dapagliflozin CAS 461432-25-7 is suitable for use in pharmaceutical synthesis, minimizing downstream purification challenges and supporting regulatory filings.

Detailed Manufacturing Process Flow for Acetyl Dapagliflozin

The synthesis of Acetyl Dapagliflozin CAS 461432-25-7 involves a multi-step organic chemistry process, optimized for yield, purity, and scalability. This manufacturing process adheres to strict quality control standards, often aligning with cGMP (current Good Manufacturing Practice) principles even for intermediates, to ensure product consistency and traceability.

Key Process Steps:

1. Step 1: Raw Material Sourcing and Qualification:

   High-quality, pre-qualified starting materials (e.g., substituted benzene derivatives, saccharide precursors) are sourced from approved vendors. Each batch undergoes rigorous incoming quality control testing against established specifications (e.g., purity by GC/HPLC, water content, heavy metals) to minimize impurities entering the synthesis chain. This critical initial step is governed by ISO 9001 and often internal pharmaceutical quality system standards.

2. Step 2: Key Intermediate Synthesis (e.g., Glucoside Precursor):

   This typically involves a Friedel-Crafts acylation or related coupling reaction between a protected glucose derivative and a halogenated aryl compound. This step is crucial for establishing the basic carbon skeleton. Reaction conditions (temperature, pressure, catalysts, solvent system) are carefully controlled and monitored. [Starting Material A] + [Starting Material B] --(Catalyst, Solvent, Heat)--> [Intermediate 1]

3. Step 3: Acetylation:

   The formed glucoside intermediate undergoes acetylation. This involves reacting the hydroxyl groups with an acetylating agent (e.g., acetic anhydride, acetyl chloride) in the presence of a base or catalyst. This step protects specific hydroxyl groups, which is crucial for subsequent reactions and improves solubility, allowing for efficient purification. [Intermediate 1] + Acetic Anhydride --(Base)--> [Acetyl Dapagliflozin crude]

4. Step 4: Purification and Isolation:

   The crude Acetyl Dapagliflozin CAS 461432-25-7 is then subjected to a series of purification steps. This typically includes recrystallization from suitable solvent systems, active carbon treatment for decolorization, and filtration. Chromatographic purification (e.g., column chromatography) may be employed for higher purity requirements or to remove specific stubborn impurities. The aim is to achieve the specified purity level, usually ≥99.0% by HPLC. [Acetyl Dapagliflozin crude] --(Recrystallization, Filtration)--> [Purified Acetyl Dapagliflozin]

5. Step 5: Drying and Milling:

   The purified product is dried using appropriate techniques (e.g., vacuum drying, tray drying) to achieve the desired moisture content. Depending on downstream requirements, the material may be milled or sieved to achieve a specific particle size distribution. All these operations are performed in controlled environments to prevent contamination.

6. Step 6: Final Quality Control and Packaging:

   The final batch of Acetyl Dapagliflozin CAS 461432-25-7 undergoes comprehensive quality control testing against all specified parameters (as outlined in the Technical Specifications table). This includes HPLC for purity and impurity profiling, Karl Fischer for water content, GC for residual solvents, and potentially other tests like heavy metals, IR, NMR, and Mass Spectrometry for structural confirmation. Once approved, the product is packaged in clean, airtight container111s, labeled with batch number, manufacturing date, expiry date, and storage conditions. Packaging is designed to protect the product from light, moisture, and degradation, ensuring a service life (shelf life) typically of 2-3 years under recommended storage conditions.

Throughout the process, stringent adherence to cGMP principles ensures product quality, consistency, and traceability. Target industries for this intermediate are primarily pharmaceutical manufacturing, contract development and manufacturing organizations (CDMOs), and advanced academic/industrial research and development. The advantages in typical application scenarios include high purity minimizing downstream purification efforts, excellent batch-to-batch consistency reducing process variability, and robust stability enhancing storage and handling safety.

Application Scenarios and Technical Advantages

Acetyl Dapagliflozin CAS 461432-25-7 is not an API itself but plays a pivotal role in the production of Dapagliflozin. Its primary application scenarios revolve around large-scale pharmaceutical synthesis and advanced research.

Key Application Scenarios:

• Commercial Synthesis of Dapagliflozin API: This is the dominant application. Pharmaceutical manufacturers utilize Acetyl Dapagliflozin CAS 461432-25-7 as a high-purity intermediate, converting it in subsequent steps (e.g., deacetylation, purification) into the final Dapagliflozin API. The high purity of the intermediate significantly reduces the complexity and cost of downstream purification processes for the final API.
• Research and Development (R&D): Academic institutions and pharmaceutical R&D labs use this compound as a building block for synthesizing Dapagliflozin derivatives, exploring new synthetic routes, or developing analytical reference standards. Its well-defined structure and purity are crucial for reproducible research outcomes.
• Generic Drug Development: Companies developing generic versions of Dapagliflozin require reliable access to intermediates with established quality and competitive pricing to replicate the innovator's synthetic pathway and meet bioequivalence requirements.

Technical Advantages Offered:

• High Purity and Low Impurity Profile: Critical for avoiding the formation of undesired by-products in subsequent synthesis steps, which could lead to genotoxic impurities or reduce API yield. This translates to reduced purification costs and higher final API quality.
• Consistent Batch-to-Batch Quality: A reliable manufacturing process, adhering to stringent QC protocols, ensures uniform product characteristics across different batches. This consistency is vital for maintaining robust and predictable API manufacturing processes.
• Optimized Reactivity: The acetyl groups strategically protect specific hydroxyl functionalities, allowing for selective reactions in subsequent synthetic steps. This controlled reactivity is a cornerstone of efficient organic synthesis.
• Scalability: Suppliers focused on B2B markets ensure their synthesis process for Acetyl Dapagliflozin CAS 461432-25-7 is fully scalable from pilot batches to commercial multi-ton production, supporting varying client needs.
• Regulatory Compliance Support: Reputable suppliers provide comprehensive documentation (CoA, MSDS, process flow, impurity data) essential for regulatory submissions (e.g., DMF filings), facilitating a smoother approval process for the final API.

Vendor Comparison and Selection Criteria

Selecting the right supplier for Acetyl Dapagliflozin CAS 461432-25-7 is a strategic decision that impacts production timelines, costs, and regulatory compliance. Beyond price, several critical factors must be evaluated.

Key Comparison Factors:

Choosing a supplier for Acetyl Dapagliflozin CAS 461432-25-7 based solely on price can lead to significant downstream costs due to impurity issues, manufacturing delays, or regulatory hurdles. A holistic evaluation emphasizing quality, reliability, and support is crucial for long-term success.

Customized Solutions and R&D Support

Recognizing that standard offerings may not always meet unique client requirements, leading suppliers of Acetyl Dapagliflozin CAS 461432-25-7 often provide customized solutions and extensive R&D support.

Customization Options:

• Batch Size Flexibility: From gram-scale for early-stage R&D to multi-ton commercial quantities, suppliers can tailor production to specific project phases.
• Purity Grades: While standard purity is high, some research applications or specific regulatory pathways might require even higher or slightly varied purity profiles. Custom analytical methods can also be developed.
• Packaging Solutions: Customized packaging to meet specific client handling, storage, or transport requirements, including specialized container111 types or inert atmosphere packing.
• Particle Size Distribution: For certain formulation or process needs, specific particle size ranges may be requested and achieved through controlled milling or crystallization techniques.

R&D and Technical Support:

• Process Development & Optimization: Collaborative efforts to optimize the synthetic route of Acetyl Dapagliflozin CAS 461432-25-7 for improved yield, reduced cost, or environmental impact.
• Analytical Method Development: Assistance in developing and validating analytical methods for in-process controls or final product release, ensuring robust quality assessment.
• Impurity Profiling and Identification: Expert support in identifying and characterizing known or novel impurities, critical for regulatory submissions and process understanding.
• Technical Consultation: Access to a team of experienced organic chemists and process engineers who can provide insights into synthetic challenges, scale-up issues, and regulatory considerations.

Application Case Studies: Leveraging Quality Intermediates

The real-world impact of high-quality Acetyl Dapagliflozin CAS 461432-25-7 is best illustrated through its application in pharmaceutical manufacturing.

Case Study 1: Large-Scale API Production Optimization

A leading generic pharmaceutical manufacturer faced challenges in their Dapagliflozin API production. They were experiencing variable batch yields and higher-than-desired levels of specific impurities, leading to increased purification steps and associated costs. Upon switching their intermediate supplier for Acetyl Dapagliflozin CAS 461432-25-7 to a cGMP-compliant vendor with stringent QC, they observed significant improvements:

• Yield Improvement: A consistent 5-7% increase in the overall Dapagliflozin API yield due to the reduced impurity load and consistent reactivity of the incoming intermediate.
• Reduced Purification Costs: Elimination of an extra crystallization step, leading to 15% reduction in solvent consumption and a 10% decrease in processing time per batch.
• Enhanced Regulatory Confidence: Robust documentation from the supplier streamlined their own regulatory filings for the Dapagliflozin API.

Case Study 2: Expediting Research & Development of Novel SGLT2 Analogues

A contract research organization (CRO) specializing in drug discovery required a reliable source of Acetyl Dapagliflozin CAS 461432-25-7 for synthesizing novel SGLT2 inhibitor analogues with modified pharmacological profiles. The CRO partnered with a supplier known for its R&D support and custom synthesis capabilities.

• Accelerated Synthesis: Consistent purity and structure confirmation of the supplied intermediate allowed the CRO's chemists to proceed directly with downstream modifications without extensive incoming quality checks or re-purification.
• Access to Technical Data: The supplier provided detailed spectroscopic data (NMR, MS) and impurity profiles, which were invaluable for characterizing the synthesized analogues and troubleshooting unexpected results.
• Scalability for Lead Optimization: As promising analogues emerged, the supplier efficiently scaled up production of the intermediate to support larger-scale synthesis for preclinical testing, demonstrating seamless transition from research to development phases.

Ensuring Quality, Trustworthiness, and Compliance ( Focus)

For a critical pharmaceutical intermediate like Acetyl Dapagliflozin CAS 461432-25-7, trust, expertise, authority, and experience are not just buzzwords; they are fundamental requirements for successful partnerships in the B2B pharmaceutical sector.

Authoritativeness and Certifications:

• ISO 9001:2015 Certification: Demonstrates a robust quality management system covering all aspects of manufacturing, from design to delivery.
• Adherence to cGMP Principles: While intermediates are not always under full GMP, applying cGMP principles for cleanliness, documentation, validation, and change control ensures the highest quality.
• FDA/EMA Audit Readiness: Reputable suppliers maintain comprehensive records and systems that can withstand rigorous audits by regulatory bodies, providing confidence to their pharmaceutical clients.
• Years of Service & Partner Clients: A long track record of successful supply to major pharmaceutical companies and research institutions validates a supplier's reliability and expertise.

Trustworthiness:

Frequently Asked Questions (FAQ)

• Q: What is the typical lead time for Acetyl Dapagliflozin CAS 461432-25-7?

  A: Standard orders for in-stock quantities typically ship within 5-7 business days. For larger custom orders or non-stock items, lead times range from 4-8 weeks, depending on synthesis complexity and batch size. We recommend early communication for project planning.

• Q: What kind of quality documentation is provided?

  A: Each shipment includes a comprehensive Certificate of Analysis (CoA) detailing purity, water content, residual solvents, and other specified parameters. Material Safety Data Sheets (MSDS) are also provided. Additional documentation for regulatory support (e.g., impurity profiles, stability data, process flow diagrams) can be provided upon request and under NDA.

• Q: Do you offer samples for evaluation?

  A: Yes, we provide samples for quality evaluation and R&D purposes. Please contact our sales team with your specific requirements.

• Q: What are your warranty and return policies?

  A: We guarantee that all products meet the specifications outlined in their respective Certificates of Analysis. If a product does not meet stated specifications upon receipt and retesting, customers must notify us within 30 days of delivery. We will arrange for product return, replacement, or refund after investigation. Our commitment is to ensure product quality and customer satisfaction.

Lead Time and Fulfillment:

Our streamlined logistics and inventory management systems ensure efficient order processing. For bulk orders of Acetyl Dapagliflozin CAS 461432-25-7, we work closely with clients to establish manufacturing schedules that align with their production timelines, offering Just-In-Time (JIT) delivery options where feasible to optimize inventory costs.

Customer Support and Technical Assistance:

Our dedicated customer support team is available to assist with inquiries ranging from order status and shipping to technical specifications. Our R&D and QA departments also provide expert technical assistance for challenging synthetic problems, impurity identification, or analytical method development related to Acetyl Dapagliflozin CAS 461432-25-7.

Conclusion: The Indispensable Role of High-Quality Intermediates

Acetyl Dapagliflozin CAS 461432-25-7 is a foundational intermediate, critical for the efficient and high-quality production of Dapagliflozin API. As the demand for SGLT2 inhibitors continues to grow, driven by expanding therapeutic applications, the strategic importance of reliable, high-purity intermediates cannot be overstated. Manufacturers and researchers seeking to optimize their synthetic processes, ensure regulatory compliance, and achieve superior product quality must prioritize partnerships with suppliers who demonstrate not only technical expertise but also unwavering commitment to quality, transparency, and customer support. Investing in a high-quality intermediate like Acetyl Dapagliflozin from a reputable source translates directly into reduced development costs, faster time-to-market, and enhanced overall product integrity.

References

1. International Diabetes Federation. IDF Diabetes Atlas, 10th edition. Brussels, Belgium: International Diabetes Federation; 2021.
2. American Chemical Society. Chemical Abstracts Service (CAS) Registry.
3. Food and Drug Administration (FDA). Guidance for Industry: Q7 Good Manufacturing Practice Guidance for Active Pharmaceutical Ingredients. September 2016.
4. European Medicines Agency (EMA). ICH Guideline Q3C (R7) on impurities: Guideline for residual solvents. February 2018.
5. United States Pharmacopeia (USP). USP-NF General Chapters, various.
6. IQVIA. Global Pharma Market Trends and Forecasts. Recent reports.