Chemical Name: Tianeptine
Synonyms；Tianeptine hemisulfate monohydrate;Tianeptineacid;Tianeptine powder;COAXIL;Tianepine;TIANEPTINE;Tianeptina;Tianeotine;Brn 1232295;Tianeptinum
CBNumber:CB3217470
Molecular Formula:C21H25ClN2O4S
Molecular Weight:436.95
MDL Number:MFCD00865376
Melting point；129-131°C
storage temp. Hygroscopic, -20°C Freezer, Under inert atmosphere
solubility；Freely soluble in water, in methanol；and in methylene chloride.
form；Solid
color；White
Chemical Properties；
White Solid
Originator；
Uses；
Tianeptine is used in the treatment of reactive and neurotic depression, as well as in the treatment of anxious states.
Uses
Tricyclic compound with psychostimulant, anti-ulcer and anti-emetic properties. Antidepressant
Manufacturing Process
A solution of 27.6 g (0.16 mol) of freshly distilled ethyl 7-aminoheptanoate in 40 ml of nitromethane was added all at once and with mechanical stirring to a suspension of 26.2 g (0.08 mol) of 5,8-dichloro-10-dioxo-11- methyldibenzo[c,f]thiazepine(1,2) in 120 ml of nitromethane. The whole was heated to 55°C for 30 minutes, the solvent was then evaporated in vacuo and the residue was taken up in water. The crude ester was extracted with ether. After evaporation of the ether 36 g of crude ester were obtained, and 30 g (0.065 mol) there of were treated under reflux with a solution of 2.8 g (0.07 mol) of sodium hydroxide in 35 ml of ethanol and 25 ml of water. After one hour's refluxing, the alcohol was evaporated in vacuo. The residue was taken up in 150 ml of water.
The mixture was twice extracted with 75 ml of chloroform and the aqueous phase was evaporated in vacuo. The sodium salt was then dissolved in 150 ml of chloroform, the solution was dried over sodium sulfate and the product precipitated with anhydrous ether.
The salt was filtered off, washed with ether and dried at 50°C. 13 g of sodium 7-[8-chloro-10-dioxo-11-methyldibenzo[c,f]thiazepin-(1,2)-aminoheptanoate,melting with decomposition at about 180°C, were obtained.
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