23694-17-9

Crystalline Solid

Dopamine D2-receptor antagonist. An antipsychotic

Barnetil,Delagrange,France,1976

Dopamine D2-receptor antagonist. An antipsychotic

Dopamine D2-receptor antagonist. An antipsychotic.

A solution of 17.22 g of N-ethyl-α-aminomethylpyrrolidine in 360 ml of pyridine is placed in a 1 l balloon flask. A solution of 3.51 g of phosphorus trichloride in 40 ml of pyridine is added at ambient temperature. After the mixture has been stirred for 1 hour, 10 g of 2-methoxy-5-ethylsulfonylbenzoic acid is introduced. The mixture is heated under reflux for 4 ? hours. After cooling, the solvent is evaporated under vacuum and the residue is dissolved in 200 ml of 20% sodium hydroxide. The solution is extracted with 200 ml of chloroform.
The organic solution is dried and filtered and the solvent is evaporated under vacuum; the residue is dissolved in 150 ml of ethanol and the solution is acidified with hydrochloric acid. The hydrochloride is dried without heating and recrystallized from 100 ml of absolute ethanol. 7.2 g of N-(1-ethyl-2- pyrrolidyl-methyl-2-methoxy-5-ethylsulfonylbenzamide hydrochloride is produced. Melting point: 190°C to 193°C.

Neuroleptic