Preparation method of tianeptine sodium intermediate

Abstract

The invention belongs to the technical field of chemical synthesis and particularly relates to a preparation method of a tianeptine sodium intermediate 3,11-dichloro-6,11-dihydro-6-methyl-dibenzo[c,f][1,2] thiazepine-5,5-dioxide. The method comprises steps as follows: 3-chloro-6,11-dihydro-6-methyl-dibenzo[c,f][1,2] thiazepine-11-alcohol-5,5-dioxide is added to an organic solvent, a chloro-substituted reagent is added, the mixture is heated to have a reflux reaction, cooled to the room temperature after the reaction is finished, filtered and dried, and then the tianeptine sodium intermediate 3,11-dichloro-6,11-dihydro-6-methyl-dibenzo[c,f][1,2] thiazepine-5,5-dioxide is prepared. According to the method, industrial hydrochloric acid commonly used on the market is used as the chloro-substituted reagent, requirements for a reaction condition are not high, requirements for equipment are low, the production process is safe, controllable and environment-friendly, the industrial hydrochloric acid raw material is low in price and easy to obtain, the cost is reduced, and the method is more suitable for industrial production.

Description

technical field [0001] The invention belongs to the technical field of chemical synthesis, and in particular relates to an intermediate 3,11-dichloro-6,11-dihydro-6-methyl-dibenzo[c,f][1,2 ] The preparation method of thiazepine-5,5-dioxide. Background technique [0002] The trade name of tianuptine sodium is Datilang, and the chemical name is 7-[(3-chloro-6,11-dihydro-6-methyldibenzo[c,f][1,2]-sulfuron Zazen-11-yl)-amino]heptanoic acid S,S-dioxide sodium salt; a drug for the treatment of mental disorders produced by the French Servier International Company. This product was imported and registered in China in December 2001. It is used for the treatment of mild, moderate or severe depression, neurogenic and reactive depression, anxiety and depression of the body, especially gastrointestinal discomfort, etc. Associated anxiety disorders play a role. Tianuptine sodium is a 5-HT reuptake agonist, which can regulate the remodeling of hippocampus, amygdala and cell dendrites. I...

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Problems solved by technology

Thionyl chloride, etc. are used as chlorinated reagents. The disadvantage is that the reaction conditions are strictly anhydrous, and the hydrogen chloride, sulfur dioxide and other gases produced by the reaction need to be absorbed, which increases the cost and pollutes the environment. Post-treatment needs to evaporate excess chlorine. sulfoxide, the process is dangerous and complicated, and is not suitable for industrial production; hydrogen chloride gas, as a chlorinated reagent, needs to be transported in steel cylinders and is inconvenient for feeding and production. The production has strict requirements on reaction equipment and operation, and there are safety hazards in the production process. Pollution, not suitable for industrial production

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