4-(MethylaMino)-3-Nitrobenzoic Acid Used for Dabigatran Etexilate Mesylate

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

Basic Info

Model No.: 41263-74-5

Additional Info

Packaging: AS REQUIRED

Productivity: KGS

Brand: VOLSENCHEM

Transportation: Air

Place of Origin: CHINA

Supply Ability: 100KG

Certificate: ISO

Product Description

Dabigatran etexilate intermediate has the chemical name of 4-(MethylaMino)-3-Nitrobenzoic Acid CAS number is 41263-74-5, Use 4-(MethylaMino)-3-Nitrobenzoic Acid as raw materials for the synthesis of dabigatran etexilate are the most widely method which reported in the literature, this method has the advantage of low prices of raw materials, but 4-methylamino-3-nitrobenzoic acid and N-Ethyl 3-(pyridin-2-ylaMino)propanoate will cause vice Products during the process of condensation, it needs for recrystallization and purification in order to carry out the next reaction. In addition, the condensed product needs to be reduced to an amino group by a nitro group. This reaction requires the catalytic hydrogenation of palladium on carbon. Because hydrogen is flammable and explosive, it is dangerous to enlarge the operation of this step. So the shortcomings of this method is also more obvious. Therefore, it is still necessary to further optimize the reaction steps to explore the best reaction time and reaction temperature to control the occurrence of by-products.
Some people adjusted the first step of this synthesis reaction ,use 4-methylamino-3-nitrobenzoic acid as raw material, added SOCl2, together heated to 81-84 ° C, reflux 2 ~ 4 h, remove excess SOCl2, get the compound of 3-nitro-4-methylaminobenzoyl chloride, the method of the reaction conditions are mild, has no other by-products, the product can be directly carried out the next reaction. This greatly simplifies the operation.


Thera. Category: Antithrombotic/Blood thinners

Cas No.:41263-74-5

Synonym:Benzoic acid, 4-(MethylaMino)-3-nitro-;Dabigatran Etexilate Intermediate 5;4-(METHYLAMINO)-3-NITROBENZOIC ACID;NSC 138300;4-(MethylaMino)-3-nitrobenzoic acid 98%;

41263-74-5

Molecular Weight:196.16

Molecular formula: C8H8N2O4

Purity: ≥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:

CAS
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 
42288-26-6
N-(4-CYANO-PHENYL)-GLYCINE HPLC 99.0%  off white  
Loss on drying 1.0%
212322-56-0
3-[(3-AMINO-4-METHYLAMINO-BENZOYL)-PYRIDIN-2-YL-AMINO]-PROPIONIC ACID ETHYL ESTER HPLC 99.0% off white  
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%
211915-84-3
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  
211915-06-9
Dabigatran Etexilate HPLC 98.0%  white  
Single impurity 0.2%
Loss on drying 1.0% 
Assay 98.0%
872728-81-9
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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