864070-43-9

Basic information

• Product Name: Empagliflozin (R)-Isomer
• Synonyms: Empagliflozin (R)-Isomer;Impurities of Empagliflozin
• CAS NO: 864070-43-9
• Molecular Formula: C23H27ClO7
• Molecular Weight: 450.90928
• Mol File: 864070-43-9.mol
• Article Data: 52

Chemical Properties

• Boiling Point: 664.5±55.0 °C(Predicted)
• Appearance: /
• Density: 1.398±0.06 g/cm3(Predicted)
• PKA: 13.23±0.70(Predicted)
• CAS DataBase Reference: Empagliflozin (R)-Isomer(CAS DataBase Reference)
• NIST Chemistry Reference: Empagliflozin (R)-Isomer(864070-43-9)
• EPA Substance Registry System: Empagliflozin (R)-Isomer(864070-43-9)

Safety Data

• Hazardous Substances Data: 864070-43-9(Hazardous Substances Data)

Usage

Uses

3’’’-Epi-Empagliflozin is an impurity of Empagliflozin (E521510) which is a novel, potent and selective SGLT-2 inhibitor, improves glycaemic control and features of metabolic syndrome in diabetic rats.

Upstream product

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• 864070-18-8 4-(5-bromo-2-chlorobenzyl)phenol 
• 912917-83-0 (3R,4S,5S,6R)-2-(4-chloro-3-(4-hydroxybenzyl)phenyl)-6-(hydroxymethyl)-2-methoxytetrahydro-2H-pyran-3,4,5-triol 
• 912917-85-2 (2S,3S,4R,5R,6R)-2-(3-(4-acetoxybenzyl)-4-chlorophenyl)-6-(acetoxymethyl)tetrahydro-2H-pyran-3,4,5-triyl triacetate 
• 89-98-5 2-chloro-benzaldehyde 
• 149965-40-2 5-bromo-2-chlorobenzyl alcohol 
• 1352955-16-8 (3aS,5R,6S,6aS)-5-hydroxymethyl-2,2-dimethyltetrahydrofuro[2,3-d][1,3]dioxolane-6-ol 
• 1103738-17-5 (3aS,5R,6S,6aS)-6-hydroxy-2,2-dimethyl-3a,5,6,6a-tetrahydrofuro[2,3-d][1,3]dioxolane-5-carboxylic acid 
• 1103738-19-7 ((3aS,5R,6S,6aS)-6-hydroxy-2,2-dimethyltetrahydrofuro[2,3-d][1,3]dioxol-5-yl)(morpholin-4-yl)methanone 
• 67-56-1 methanol 
• 915095-89-5 (S)-4-bromo-1-chloro-2-(4-tetrahydrofuran-3-yloxy-benzyl)benzene 
• 32469-28-6 (3R,4S,5R,6R)-3,4,5-tris((trimethylsilyl)oxy)-6-(((trimethylsilyl)oxy)methyl)tetrahydro-2H-pyran-2-one 

Relevant articles and documents

Preparation method of SGLT-2 inhibitor and intermediate

The invention discloses a preparation method of an SGLT-2 inhibitor and an intermediate. The method comprises the following steps: (1) reacting a compound A with chlorosilane under the action of an acid-binding agent to generate a compound B; (2) mixing the compound B and a compound C to obtain a compound D; and (3) reacting the compound D with a reducing agent and a catalyst to obtain the SGLT-2 inhibitor compound.

Synthesis, Isolation, Characterization and Suppression of Impurities during Optimization of Empagliflozin (Jardiance)

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Synthetic method of empagliflozin

The invention belongs to the technical field of raw material medicine preparation, and relates to a synthetic method of an SGLT-2 inhibitor empagliflozin, which comprises the following steps: 1) taking glucose as an initial raw material, and preparing an active intermediate 3 through full acylation, selective hydrolysis and esterification; 2) reacting the intermediate 3 with chlorobenzene under the catalysis of boron trifluoride/diethyl ether to generate an intermediate 4, and reacting the intermediate 4 with paraformaldehyde and phenoxy tetrahydrofuran to generate an intermediate 5; and 3) removing the protecting group under the action of alkali to obtain the final product empagliflozin. The method is simple to operate, low-temperature reaction in the prior art is avoided, and the purity of the obtained product is higher.