872728-85-3,Intermediates of Dabigatran Etexilate

Payment Type: L/C,T/T
Incoterm: FOB
Min. Order: 1 Kilogram
Delivery Time: 15 Days

Basic Info

Model No.: 872728-85-3

Additional Info

Packaging: AS REQUIRED

Productivity: KGS


Transportation: Air

Place of Origin: CHINA

Supply Ability: 100KG

Certificate: ISO

Product Description

Dabigatran etexilate intermediate has the chemical name of N-[[2-[[[4-(AMinoiMinoMethyl)phenyl]aMino]Methyl]-1- Methyl-1H- benziMidazol-5-yl] carbonyl]-N-2-pyridinyl-beta-alanine ethyl ester 4-MethylbenzenesulfonateCAS number is 872728-85-3, which is the N-1 step intermediate of dabigatran etexilate mesylate. His preparation process is as follows: 47.7 g of ethyl dabigatran etexilate, 21.8 g of p-toluenesulfonic acid and 142 g of a 10 mol / L hydrogen chloride ethanol solution were sequentially added to a 1000 mL glass reaction flask,. The reaction solution was incubated at room temperature for 24 hours. Add 400ml Ethanol into the solution.cooled the temperate to 0℃,slowing inlet ammonia, . After the precipitate was completely  then heated to 10 ° C, the mixture was incubated for 2 hours and then warmed to room temperature overnight. The solvent was evaporated under reduced pressure, add 400ml ethanol, 400mL of water was added dropwise with stirring, sodium hydroxide 2.3g was added and the temperature was raised to 55 ° C ,incubated for 45 minutes. After finished,The mixture was cooled to 10 ° C and stirred for 1 hour. The mixture was filtered and the filtrate was distilled under reduced pressure to remove ethanol. The solid was precipitated, filtered, washed once with 200 mL of water, twice with 100 mL of acetone and dried with air at 55 ° C to get 34.6gram off white solid., The white solid is the target compound dabigatran etexilate mesylate N-1 cas 872728-85-3. Product purity was 85%. Since dabigatran etexilate mesylate is difficult to remove impurities by purification, the number of unknown single impurities of dabigatran etexilate mesylate N-1 intermediate and purity result decide the quality of dabigatran etexilate mesylate. Therefore, improved the purification method,make the purity more than 95% pure andother unknown single impurity less than 0.15%, then the dabigatran etexilate mesylate meets the quality requirements of the original drug manufacturers.

Thera. Category: Antithrombotic/Blood thinners

Cas No.:872728-85-3

Synonym:Ethyl 3-(2-(((4-carbaMiMidoylphenyl)aMino)Methyl)-1-Methyl-N-(pyridin-2-yl)-1H-benzo[d]iMidazole-5-carboxaMido)propanoate 4-Methylbenzenesulfonate;Dabigatran ethyl ester tosylate


Molecular Weight:777.88628

Molecular formula: C27H29N7O3.C7H8O3S

Assay: ≥98.%

Appearance: White Crystalline solid

Packing:Export worthy packing

Material Safety Data Sheet:Available on request

Usage: It can treat and prevent blood clots, reducing the risk of stroke.

Related intermediate:

Chemical Name Specification Color
41263-74-5 4-(MethylaMino)-3-nitrobenzoic acid HPLC 99.0% pale brown
           103041-38-9 N-[2]PYRIDYL-B-ALANIN-ETHYL ESTER HPLC 99.0% off white to white
           429659-01-8 ETHYL N-[4-(METHYLAMINO)-3-NITROBENZOYL]-N-PYRIDIN-2-YL-SS-ALANINATE HPLC 99.0% orange yellow solid 
N-(4-CYANO-PHENYL)-GLYCINE HPLC 99.0%  off white  
Loss on drying 1.0%
Melting point 101.0°C~106.0°C
Single impurity 0.3% 
Loss on drying 0.5%
Residue on ignition 0.5% 
Assay 98.0%
Synonyms:3-[[[2-[[(4-Cyanophenyl)amino]methyl]-1-methyl-1H-benzimidazol-5-yl]carbonyl]pyridin-2-ylamino]propionic acid ethyl ester HPLC 99.0% off white  
Single impurity 0.3%
Loss on drying 0.5% 
Residue on ignition 0.5% 
Assay 99.0%
 872728-85-3 N-[[2-[[[4-(Aminoiminomethyl)phenyl]amino]methyl]-1-methyl-1H-benzimidazol-5-yl]arbonyl]-N-2-pyridinyl-beta-alanine ethyl ester 4-methylbenzenesulfonate HPLC 97.0% off white  
Dabigatran Etexilate HPLC 98.0%  white  
Single impurity 0.2%
Loss on drying 1.0% 
Assay 98.0%
Dabigatran etexilate mesylate HPLC 99.0%  light yellow solid
Single impurity 0.5%
Loss on drying 1.0% 
Residue on ignition 0.1% 
Heavy melta 20 ppm 
Assay 98.5%

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