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| Product Information |
Product name | Empagliflozin Intermediate (3S)-3-[4-[(5-Bromo-2-chlorophenyl)methyl]phenoxy]tetrahydrofuran |
Synonyms | Empagliflozin int3; Empagliflozin-7; Empagliflozin Bromo Impurity; (S)-4-bromo-1-chloro-2-(4-tetrahydrofuran-3-yloxy-benzyl)-benzene; 3-[4-[(5-broMo-2-chlorophenyl)Methyl]phenoxy]tetrahydro-; (3S)-3-(4-(5-Bromo-2-chlorobenzyl)phenoxy)tetrahydro-furan; (3S)-3-[4-[(5-bromo-2-chlorophenyl)methyl]phenoxy]oxolane 915095-89-5 |
CAS | 915095-89-5 |
Molecular Formula | C17H16BrClO2 |
Molecular Weight | 367.66 |
Molecular Structure |
|
Quality Standard | 99% up by HPLC |
Appearance | White to off-white powder |
| Empagliflozin Intermediate – Core Technology for SGLT2 Inhibitor Synthesis |
Empagliflozin (CAS 915095-89-5), a leading global SGLT2 inhibitor for diabetes treatment, relies on the precise synthesis and quality control of key intermediates to ensure its efficacy and safety. This article focuses on the chemical structure, production process, and impurity control of Empagliflozin intermediates, exploring their core value in the field of SGLT2 inhibitor intermediates.
| Core Process: Targeted Synthesis of High-Purity Intermediates |
1. Chemical Structure and Synthesis Route of Key Intermediates
The chemical structure of Empagliflozin intermediate is based on a phenyl glucoside core, built through multiple reaction steps:
- Step 1: 2-chloro-5-iodobenzoic acid is used as the starting material for the Suzuki coupling reaction, introducing the aryl fragment.
- Step 2: Glycosylation reaction connects the D-glucose unit, forming Empagliflozin 7 intermediate (key intermediate C7).
- Step 3: Construction of the chiral center and deprotection, ensuring the stereoselectivity of the final product (ee value > 99.5%).
2. Green Synthesis Process Optimization
- Continuous Flow Technology: Replaces traditional batch reactions, reducing the Empagliflozin intermediate production cycle by 40% and reducing solvent usage.
- Enzyme Catalysis: Immobilized enzymes are used in the glycosylation step to improve reaction efficiency and avoid metal residue.
- Crystallization Purification: A solvent gradient crystallization method is used, achieving intermediate purity of ≥99.8%, meeting GMP standards for pharmaceutical intermediates for Empagliflozin.
| Quality Assurance: Impurity Research and Process Control |
1. Empagliflozin Impurity Tracking and Control
- Genotoxic Impurities: LC-MS/MS is used to monitor halogenated by-products that may be generated during synthesis (e.g., Empagliflozin impurity 915095-89-5 synthesis-related impurities), with a limit of <10 ppm.
- Chiral Impurities: Chiral HPLC monitors enantiomer excess (ee value) to ensure compliance with ICH Q3A requirements.
2. Comprehensive Process Analytical Technology
- HPLC-DAD/ELSD: Real-time monitoring of intermediate purity and main component content.
- NMR and HRMS: Confirm the accuracy of the Empagliflozin intermediate chemical structure.
- Elemental Analysis: Control heavy metal (Pb, As) residue to <1 ppm.
| Process Advantages and Customer Value |
1. Customized Supply Capability
- Provides Empagliflozin intermediates for sale, including key intermediates such as C3, C5, C7.
- Supports process development and scale-up (from gram to ton scale), shortening the customer’s drug registration cycle.
2. Compliance and Cost Advantage
- Meets FDA/EMA requirements for SGLT2 inhibitor intermediates in API registration (DMF document support).
- Integrated production reduces the cost of Empagliflozin 7 intermediate production process (C7 intermediate production) by more than 30%.
| Product Information |
Product name | Empagliflozin Intermediate (3S)-3-[4-[(5-Bromo-2-chlorophenyl)methyl]phenoxy]tetrahydrofuran |
Synonyms | Empagliflozin int3; Empagliflozin-7; Empagliflozin Bromo Impurity; (S)-4-bromo-1-chloro-2-(4-tetrahydrofuran-3-yloxy-benzyl)-benzene; 3-[4-[(5-broMo-2-chlorophenyl)Methyl]phenoxy]tetrahydro-; (3S)-3-(4-(5-Bromo-2-chlorobenzyl)phenoxy)tetrahydro-furan; (3S)-3-[4-[(5-bromo-2-chlorophenyl)methyl]phenoxy]oxolane 915095-89-5 |
CAS | 915095-89-5 |
Molecular Formula | C17H16BrClO2 |
Molecular Weight | 367.66 |
Molecular Structure |
|
Quality Standard | 99% up by HPLC |
Appearance | White to off-white powder |
| Empagliflozin Intermediate – Core Technology for SGLT2 Inhibitor Synthesis |
Empagliflozin (CAS 915095-89-5), a leading global SGLT2 inhibitor for diabetes treatment, relies on the precise synthesis and quality control of key intermediates to ensure its efficacy and safety. This article focuses on the chemical structure, production process, and impurity control of Empagliflozin intermediates, exploring their core value in the field of SGLT2 inhibitor intermediates.
| Core Process: Targeted Synthesis of High-Purity Intermediates |
1. Chemical Structure and Synthesis Route of Key Intermediates
The chemical structure of Empagliflozin intermediate is based on a phenyl glucoside core, built through multiple reaction steps:
- Step 1: 2-chloro-5-iodobenzoic acid is used as the starting material for the Suzuki coupling reaction, introducing the aryl fragment.
- Step 2: Glycosylation reaction connects the D-glucose unit, forming Empagliflozin 7 intermediate (key intermediate C7).
- Step 3: Construction of the chiral center and deprotection, ensuring the stereoselectivity of the final product (ee value > 99.5%).
2. Green Synthesis Process Optimization
- Continuous Flow Technology: Replaces traditional batch reactions, reducing the Empagliflozin intermediate production cycle by 40% and reducing solvent usage.
- Enzyme Catalysis: Immobilized enzymes are used in the glycosylation step to improve reaction efficiency and avoid metal residue.
- Crystallization Purification: A solvent gradient crystallization method is used, achieving intermediate purity of ≥99.8%, meeting GMP standards for pharmaceutical intermediates for Empagliflozin.
| Quality Assurance: Impurity Research and Process Control |
1. Empagliflozin Impurity Tracking and Control
- Genotoxic Impurities: LC-MS/MS is used to monitor halogenated by-products that may be generated during synthesis (e.g., Empagliflozin impurity 915095-89-5 synthesis-related impurities), with a limit of <10 ppm.
- Chiral Impurities: Chiral HPLC monitors enantiomer excess (ee value) to ensure compliance with ICH Q3A requirements.
2. Comprehensive Process Analytical Technology
- HPLC-DAD/ELSD: Real-time monitoring of intermediate purity and main component content.
- NMR and HRMS: Confirm the accuracy of the Empagliflozin intermediate chemical structure.
- Elemental Analysis: Control heavy metal (Pb, As) residue to <1 ppm.
| Process Advantages and Customer Value |
1. Customized Supply Capability
- Provides Empagliflozin intermediates for sale, including key intermediates such as C3, C5, C7.
- Supports process development and scale-up (from gram to ton scale), shortening the customer’s drug registration cycle.
2. Compliance and Cost Advantage
- Meets FDA/EMA requirements for SGLT2 inhibitor intermediates in API registration (DMF document support).
- Integrated production reduces the cost of Empagliflozin 7 intermediate production process (C7 intermediate production) by more than 30%.
