Empagliflozin Basic Product Information

Product Name	Empagliflozin	CAS	864070-44-0
Synonyms	(2S,3R,4R,5S,6R)-2-(4-chloro-3-(4-((S)-tetrahydrofuran-3-yloxy)benzyl)phenyl)-6-(hydroxyMethyl)-tetrahydro-2H-pyran-3,4,5-triol;Empaglifloin;Glyxambi;mpagliflozin;(1S)-1,5-Anhydro-1-C-[4-chloro-3-[[4-[[(3S)-tetrahydro-3-furanyl]oxy]phenyl]methyl]phenyl]-D-glucitol;ozin;Empag;CS-798;EmpagL;BI-10773	Molecular Formula	C23H27ClO7
EINECS Number	620-176-8	Molecular Structure
Appearance	Light Yellow Powder
Purity
Supply Ability

Empagliflozin Quality documents

Empagliflozin Appearance/Package/Shipping/Storage

package

storage condition

Store in cool & dry place,Keep away from strong light and heat

Empagliflozin Application

Empagliflozin literature

Preparation method of SGLT-2 inhibitor and intermediate

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, (2021/05/19)

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)

Liu, Xiao,Peng, Peng,Yang, Jiangtao,Yu, Jun,Zhang, Fuli,Zhao, Chuanmeng

, (2022/03/14)

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IMPROVED PROCESS FOR THE PREPARATION OF EMPAGLIFLOZIN AND ITS CRYSTALLINE POLYMORPH

-

, (2021/12/31)

The present invention relates to an improved method for the production of Empagliflozin formula (I). The invention further relates to the preparation of a crystalline form of Empagliflozin and its particle size having a coarser particle or a D₅₀ equal to or greater than 60 μm and a D₉₀ equal to or greater than 180 μm. (I)

Synthetic method of empagliflozin

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Paragraph 0039; 0041-0042; 0044, (2021/10/30)

The invention discloses a synthesis method of empagliflozin. According to the method, (S)-3-(4-(5-bromo-2-chlorobenzyl) phenoxy) tetrahydrofuran is adopted as a starting raw material and is coupled with 2, 3, 4, 6-tetrabenzyl-D-glucopyranosyl-1, 5-lactone under the catalysis of Pd2 (dba) 3 and the combined action of p-toluenesulfonhydrazide, Xphos and lithium tert-butoxide to generate an intermediate I, double bonds of the intermediate I are subjected to hydrogenation reduction through raney nickel, meanwhile, debenzylation is conducted, and the empagliflozin is obtained. The method does not need butyl lithium, Grignard reagent and other dangerous materials, has the advantages of short reaction route, simple reaction and post-treatment, high safety, few side reactions, high product yield and high purity, and is especially suitable for industrial production.

Empagliflozin Upstream and downstream

864070-44-0 Upstream product

• 864070-37-1

  (2S,3R,4R,5S,6R)-2-(4-chloro-3-(4-hydroxybenzyl)phenyl)-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol 

• 219823-47-9

  (R)-tetrahydrofuran-3-yl 4-methylbenzenesulfonate 

• 915095-96-4

  methyl-1-C-(4-chloro-3-{4-[(3S)-tetrahydrofuran-3-yloxy]benzyl}phenyl)-D-glucopyranoside 

• 1279691-36-9

  (2S,3R,4S,5S,6R)-2-(4-chloro-3-(4-(((S)-tetrahydrofuran-3-yl)oxy)benzyl)phenyl)-6-(hydroxymethyl)-2-methoxytetrahydro-2H-pyran-3,4,5-triol 

• 462-06-6

  fluorobenzene 

• 19094-56-5

  2-chloro-5-iodobenzoic acid 

• 915095-94-2

  (3S)-3-[4-[(2-chloro-5-iodophenyl)methyl]phenoxy]tetrahydrofuran 

• 32469-28-6

  (3R,4S,5R,6R)-3,4,5-tris((trimethylsilyl)oxy)-6-(((trimethylsilyl)oxy)methyl)tetrahydro-2H-pyran-2-one 

864070-44-0 Downstream Products

• 915095-99-7

  (2R,3R,4R,5S,6S)-2-(acetoxymethyl)-6-(4-chloro-3-(4-(((S)-tetrahydrofuran-3-yl)oxy)benzyl)phenyl)tetrahydro-2H-pyran-3,4,5-trityl triacetate 

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