Technique for synthesizing Irbesartan

Abstract

A process for synthesizing Ebeishatan features that the intermediate 2-n-butyl-3-[(2'-cyanobiphenyl-4- yl)methyl]-1,3-diazaspiro [4,4]-nonyl-1-ene-4-one can be directly used in next step without purification, and in the reaction where cyano is converted to tetrazazole, the mixture of tributyl tin chloride and sodium azide is used to replace tributyl tin azide. Its advantage is high output rate up to 75%.

Description

technical field [0001] The invention relates to a synthesis process of irbesartan. Background technique [0002] Regarding the synthesis technique of irbesartan, the existing public literature reports are based on 2-n-butyl-1,3-diazaspiro[4,4]-non-1-en-4-one (hereinafter referred to as hetero Ring) is condensed with 4-bromomethyl-2′-cyano-biphenyl to give 2-n-butyl-3-[(2’-cyanobiphenyl-4-yl)methyl]-1,3- Diazaspiro[4,4]-non-1-en-4-one, the compound is prepared by reacting with tri-n-butyl tin azide. The intermediate 2-n-butyl-3-[(2'-cyanobiphenyl-4-yl)methyl]-1,3-diazaspiro[4,4]-nonan-1- The purification method of en-4-one is column chromatography separation, which is not suitable for industrial production, and the raw material tri-n-butyltin azide is difficult to purchase in China. Contents of the invention [0003] The technical problem to be solved by the present invention is that the existing irbesartan syn...

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Problems solved by technology

[0003] The technical problem to be solved by the present invention is that the existing irbesartan synthesis process is not suitable for industrial production, the production cost is high, and the raw materials are rare.