| This paper is the study on the synthetic process of antidepressant Tianeptine Sodium.Chapter 1 Introduction.Briefly introduced the research background of Tianeptine Sodium.Chapter 2 Summarized the synthetic routes.Based on two key intermediates,and introduce the synthetic routes in three parts.The first key intermediate,methyl 4-chloro-2-(N-methyl-N-phenylsulphonamide)benzoate.Analyzed the literature ROS,which mentioned the costly and uncommon raw materials,long and not eco-friendly synthesis step,confirm our raw material and ROS.The second key intermediate,3,11-dichloro-6,11-dihydro-6-methyl-5,5-dioxodibenzo[c,f][1,2]thiazepine.There are a few steps from the first to second,and a small difference among them.Based on the common raw material and safe reaction,the ROS of side chain 7-aminoheptanate reacting with key intermediate to get the API,was preferred.Chapter 3 Improve the selected ROS,on the principle of safer,more eco-friendly,more industrialized.Intermediate A,methyl 4-chloro-2-(N-methyl-N-phenylsulphonamide)benzoate was produced from 2-amino-4-chlorobenzoic acid after esterification,diazotization,sulfonylation and amination,some reagents were removed and replaced during the process..Intermediate B,3,11-dichloro-6,11-dihydro-6-methyl-5,5-dioxodibenzo[c,f][1,2]thiazepine was synthesized after hydrolysis,chlorination,cyclization,reduction and chlorination from Intermediate A.And the related reaction cyclization and chlorination were improved.High purity Tianeptine Acid was gotten by the reaction of intermediate B with 7-aminoheptanoic acid.After salt forming reaction,Tianeptine Sodium was formed.Chapter 4 Detailed description of the experimental process,technological optimization of the improved points,confirmed the related reaction conditions,analyse and test the intermediates and products of each step.Through a series of improvements,finally arrived the destination of more eco-friendly,lower cost,less energy consumption and more suitable for industrialization. |
PDF Full Text Request