1354727-65-3

Upstream product

• 1188417-09-5 1-methyl-2-[N-(4-cyanophenyl)aminomethyl]benzimidazole-5-ylcarboxylic acid N-(2-pyridyl)-N-(2-ethoxycarbonylethyl)amide acetate salt 
• 64-17-5 ethanol 
• 211915-84-3 3-[[[2-[[(4-cyanophenyl)amino]methyl]-1-methyl-1H-benzimidazol-5-yl]carbonyl](pyridin-2-yl)amino]propionic acid ethyl ester 
• 42288-26-6 (4-cyanophenyl)glycine 
• 212322-56-0 ethyl 3-{[{2-amino-1-(methylamino)phen-4-yl}carbonyl](pyridyn-2-yl)amino}propanoate 
• 1422469-70-2 ethyl 3-[[2-[(4-cyanophenylamino)methyl]-1-methyl-1H-benzimidazole-5-carbonyl]pyridin-2-yl-amino]propionate succinic acid 

Downstream Products

• 429658-95-7 3-({2-[(4-carbamimidoylphenylamino)methyl]-1-methyl-1H-benzoimidazole-5-carbonyl}pyridin-2-yl-amino)propionic acid ethyl ester 
• 211915-06-9 dabigatran etexilate 

Relevant academic research and scientific papers

Improved method for preparing dabigatran etexilate intermediate

The invention belongs to the field of medical intermediate synthetic methods, and relates to an improved method for preparing a dabigatran etexilate intermediate, in particular, a synthetic method of3-[[[2-[[(4-amidinophenyl)amino]methyl]-1H-benzimidazole-5-yl]carbonyl](pyridine-2-yl)amino] ethyl propionate p-toluene sulfonate 1. According to the method, use of a large amount of solvents and hydrogen chloride is avoided, the reaction process is stable, the dosage of reactants is easy to control, on one hand, impurities generated by side reactions are reduced, and subsequent synthesized dabigatran etexilate is easier to purify; on the other hand, wastes caused by release of saturated hydrogen chloride gas are greatly reduced, the environmental pollution is reduced, meanwhile the steps aresimple and easy to control, and the method is suitable for large-scale production.

METHOD FOR MANUFACTURING DABIGATRAN ETEXILATE

Disclosed is a method for producing dabigatran etexilate. The method for producing dabigatran etexilate according to one embodiment of the present invention comprises: a first step of reacting a compound of chemical formula 1 with a chlorine-based compound to synthesize a compound of chemical formula 2; a second step of reacting the compound of the chemical formula 2 with an ammonium-based compound to synthesize a compound of chemical formula 3; and a third step of reacting the compound of the chemical formula 3 with a chloroformate-based compound.COPYRIGHT KIPO 2017

Preparation method of alkaline liquor of high concentration and application thereof

The invention relates to a preparation method of alkaline liquor of high concentration. The preparation method concretely comprises the following steps: a proper amount of a solubilizer and a phase-transfer catalyst are added into an organic phase; a modi

IMPROVED PROCESSES FOR THE PREPARATION OF DABIGATRAN ETEXILATE USING NOVEL INTERMEDIATES

Disclosed herein are novel, commercially viable and industrially advantageous processes for the preparation of Dabigatran or a salt thereof, in high yield and purity, using novel intermediate compounds. The novel process solves the drawbacks associated with the prior processes and is commercially viable for preparing Dabigatran and its salts or derivatives thereof.

SYNTHESIS PROCESS OF DABIGATRAN ETEXILATE MESYLATE, INTERMEDIATES OF THE PROCESS AND NOVEL POLYMORPH OF DABIGATRAN ETEXILATE

12956PTWO_eng 23 "SYNTHESIS PROCESS OF DABIGATRAN ETEXILATE MESYLATE, INTERMEDIATES OF THE PROCESS AND NOVEL POLYMORPH OF DABIGATRAN ETEXILATE" Abstract A novel process is described for the production of Dabigatran etexilate mesylate, a 5 compound having the following structural formula: and two novel intermediates of said process.

Synthesis, characterization and suppression of impurities during optimization of dabigatran etexilate

The synthetic methods for two impurities of dabigatran etexilate are firstly described, and both of two impurities are characterized by NMR and MS spectral data. The suppression of impurities as well as the optimization process of dabigatran etexilate is also disclosed.