1449029-77-9

Upstream product

• 1397836-49-5 1-[(2'-(N'-hydroxycarbamimidoyl)[1,1'-biphenyl]-4-yl)methyl]-2-ethoxy-1H-1,3-benzodiazole-7-carboxylic acid 
• 80841-78-7 4-chloromethyl-5-methyl-1,3-dioxol-2-one 
• 147403-65-4 methyl 2-ethoxy-1-((2′-(N′-hydroxycarbamimidoyl)-biphenyl-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate 
• 139481-44-0 methyl 1-[(2'-cyanobiphenyl-4-yl)methyl]-2-ethoxy-benzimidazole-7-carboxylate 
• 76-83-5 trityl chloride 

Downstream Products

• 863031-21-4 Azilsartan medoxomil 
• 1449029-78-0 (5-methyl-2-oxo-1,3-dioxol-4-yl) methyl 2-ethoxy-1-[(2'-{N'-[(ethoxycarbonyl)oxy]carbamimidoyl}-biphenyl-4-yl)-methyl]-1H-benzimidazole-7-carboxylate 
• 1449029-80-4 (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 2-ethoxy-1-{[2'-(N'-{[(4-nitrophenoxy)carbonyl]oxy}carbamimidoyl)biphenyl-4-yl]methyl}-1H-benzimidazole-7-carboxylate 

Relevant academic research and scientific papers

arab League Qi Shatan ester or its salt synthetic method and intermediates thereof, and method for synthesizing intermediate (by machine translation)

The invention relates to the field of medicines and in particular relates to a synthesis method for azilsartan medoxomil or salt thereof, an intermediate of the azilsartan medoxomil or the salt thereof and a synthesis method for the intermediate. According to the novel method for the azilsartan medoxomil or the salt thereof, the problems of low synthesized azilsartan medoxomil yield and large number of byproducts are solved. Furthermore, the invention further provides a synthesis intermediate of the azilsartan medoxomil or the salt thereof and two preparation methods. In a synthesis process, an alcohol fragment of the azilsartan medoxomil is introduced at first, so that a part of the azilsartan medoxomil is formed, and a cyclization structure fragment is synthesized; therefore, the problem that the yield is reduced because of side reaction caused by active hydrogen in a carbonyldimidazole structure of an azilsartan acid structure is solved in a reaction process; the reaction yield is greatly improved, so that a finished product is easier to purify; the synthesis method is particularly suitable for industrial production.

PROCESS FOR THE PREPARATION OF AZILSARTAN MEDOXOMIL OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF

The present invention relates to a process for the preparation of azilsartan medoxomil or pharmaceutically acceptable salts thereof.

Commercial synthesis of azilsartan kamedoxomil: An angiotensin II receptor blocker

A commercially viable process for the preparation of azilsartan kamedoxomil, an angiotensin II receptor blocker, has been developed. The present work describes the novel synthesis of azilsartan medoxomil from amidoxime methyl ester. The present work also describes the improved synthesis of amidoxime methyl ester and azilsartan kamedoxomil. This process features a high overall yield (36%) with 99.52% HPLC purity.

PROCESS FOR THE PREPARATION OF AZILSARTAN MEDOXOMIL OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF

The present invention relates to a process for the preparation of azilsartan medoxomil or pharmaceutically acceptable salts thereof.