Blood Thinners Dabigatran Etexilate Mesylate Intermediate 212322-56-0

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

Basic Info

Model No.: 212322-56-0

Additional Info

Packaging: AS REQUIRED

Productivity: KGS


Transportation: Air

Place of Origin: CHINA


Certificate: ISO

Product Description

The N-3 intermediate of dabigatran etexilate, CAS number is 212322-56-0, abbreviated as dabigatran etexilate N-3. His preparation process is as follows: 38.9g of ethyl 3- (pyridin-2-ylamino) propionate and 37.3g of 1- (3-dimethylaminopropyl) -3-ethylcarbodiimide were dissolved in 500mL of dimethyl chloride, 39.2 g of 4-methylamino-3-nitrobenzoic acid and 38.8 g of N, N-diisopropylethylamine were added in lots at room temperature for 18 hours and monitored by TLC. After the reaction was completed, the solvent was removed under reduced pressure and dissolved with  appropriate amount of ethyl acetate, washed with saturated sodium bicarbonate, saturated brine, dried over anhydrous sodium sulfate, filtered and concentrated. The residue was dissolved in ethyl acetate, the dried hydrogen chloride was passed through the solution until the solution   was completely precipitated and filtered and dried , get the target crude compound dabigatran etexilate N-3 intermediate CAS 212322-56-0,. Then 1: 1 mixture of ethanol - acetonitrile was heated to dissolve, slowly cooled to 10 ° C, keep crystal for 2 hours, filtered and dried to get refined dabigatran etexilate N-3 intermediate 78.7g. The calculated yield was 95.2%. Product purity by HPLC was 99%.

Thera. Category: Antithrombotic/Blood thinners

Cas No.:212322-56-0

Synonym :Ethyl 3-{1-[3-aMino-4-(MethylaMino)-phenyl]-N-(pyridin-2-yl)-forMaMido}-propanoate;ethyl (2S)-2-{1-[3-aMino-4-(MethylaMino)phenyl]-N-(pyridin-2-yl)forMaMido}propanoate;3-[3-aMino-4-(MethylaMinobenzoyl)-pyridin-2-ylaMni] propionic acid ethyl ester;Ethyl N-[3-aMino-4-(MethylaMino)benzoyl]-N-pyridin-2-yl-beta-alaninate;3-[(3-AMINO-4-METHYLAMINO-BENZOYL)-PYRIDIN-2-YL-AMINO]-PROPIONIC ACID ETHYL ESTER;N-[3-amino-4-(methylamino)benzoyl]-N-2-pyridinyl-β-Alanine,ethylester;Ethyl 3-(3-amino-4-(methylamino)-N-(pyridin-2-yl)benzamido)propanoate;Dabigatran Intermediate 1;


Molecular Weight: 342.39228

Molecular formula: C18H22N4O3

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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