CAS 211915-84-3,Intermediate for Dabigatran Etexilate Mesylate

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

Basic Info

Model No.: 211915-84-3

Additional Info

Packaging: AS REQUIRED

Productivity: KGS


Transportation: Air

Place of Origin: CHINA


Certificate: ISO

Product Description

The N-2 step intermediate of Dabigatran etexilate CAS number is 211915-84-3, the appearance of white powder. we refer to it as dabigatran etexilate intermediate N-2. we found in the study that the existing technology of dabigatran etexilate intermediate N-2 has many defects, such as it needs to obtain under violent reaction conditions,but the product contains many more impurities. It must be purified by column chromatography directly or by column chromatography after it is dissociated, then proceed with the next reaction. There is a more reliable method, the target compound can be obtained after 3 steps, details as follows:
(1), 20g methyl 3-methoxy-4-aminobenzoate was added into a 500ml reaction flask, 200ml of tetrahydrofuran and 30.6ml of triethylamine were added, the temperature was lowered to 0 ° C and 15.6g of methyl iodide was slowly added dropwise for 30min, the reaction was stirred at 5 ° C for 3h after dropping, warmed to 25 ° C, stirred with 100ml of saturated aqueous ammonium chloride solution for 15min, separated into layers ,get the organic phase, washed twice with 150ml of ethyl acetate. The organic phases were combined, The solvent was evaporated under reduced pressure to get the solid, which was dried at 65 ° C under 0.08 MPa vacuum for 2 h to obtain 18.7 g of the corresponding methyl benzoate.
(2) 18.7g of the methyl benzoate compound obtained in the first step was added to the reaction flask, 100ml of ethyl acetate was added, and 18.6g of ethyl 3- (pyridin-2-ylamino) propionate was dissolved in 50ml Ethyl acetate, then added to the reaction solution, stirred at room temperature for 12hours, the solvent was evaporated under reduced pressure (vacuum: 0.075Mpa; temperature: 50 ℃) to obtain a solid, dried at 65 ℃ vacuum 0.08Mpa for 2hours,get the corresponding acrylic acid ester compound 27.7 g.
(3) 27.7 g of the ethyl acrylate compound obtained in the second step was added to the reaction flask, and 200 ml of ethyl acetate, 13.6 g of 2- (4-cyanophenylamino) acetamide, 6.2 g of carbonyldiimidazole , 4.6g of glacial acetic acid were added by turn.the reaction mixture was heated to 50 ° C and stirred for 6h. After the reaction was over, the mixture was washed with 100ml of saturated sodium carbonate. The organic layers were separated and the solvent was removed under reduced pressure to give a solid. Add 370ml of anhydrous ethanol in the residue substance , heated to dissolve, headed till it was dissolved,, then filtered, cooled temperature naturally and crystallization for 5h, filtered and vacuum dried for 5h (vacuum 0.09Mpa, 50 ° C) to give the target product 25.4gram dabigatran etexilate N-2 Step CAS number 211915-84-3,.

Thera. Category: Antithrombotic/Blood thinners

Cas No.:211915-84-3

Synonym Ethyl 3-[[[2-[[(4-Cyanophenyl)aMino]Methyl]-1-Methyl-1H-benziMidazol-5-yl]carbonyl]pyridin-2-ylaMino] propionate;Ethyl N-[(2-{[(4-cyanophenyl)aMino]Methyl}-1-Methyl-1H-benziMidazol-5-yl)carbonyl]-N-pyridin-2-yl-beta-alaninate;:3-[[[2-[[(4-Cyanophenyl)amino]methyl]-1-methyl-1H-benzimidazol-5-yl]carbonyl]pyridin-2-ylamino]propionic acid ethyl ester;Ethyl 3-(2-((4-cyanophenylamino)methyl)-1-methyl-N-(pyridin-2-yl)-1H-benzo[d]imidazole-5-carboxamido;Dabigatran Intermediate 3;Ethyl 3-(2-((4-cyanophenylaMino)Methyl)-1-Methyl-N-(pyridin-2-yl)-1H-benzo[d]iMi;Ethyl 3-(2-((4-cyanophenylaMino)Methyl)-1-Methyl-N-(pyridin-2-yl)-;3-[[[2-[[(4-Cyanophenyl)aMino]Methyl]-1-Methyl-1H-benziMidazol-5-yl]carbonyl]pyridin-2-ylaMino]propi;


Molecular Weight: 482.53

Molecular formula: C27H26N6O3

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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