NEW IMIDAZOLINE COMPOUND, METHOD OF PREPARATION, AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME

摘要

PURPOSE: A new imidazoline compound is provided, which inhibits re-absorption of 2-adrenergic antagonist and monoamine(serotonin and/or noradrenalin), so which can be used in a much more effective anti-melancholia medicine. A manufacturing process of the new imidazoline compound, and a pharmaceutical composition containing same are also provided. CONSTITUTION: A process for the preparation of 4-(3,4-dihydro-2-naphtylmethyl)4,5-dihydro-1H-imidazole fumarate(a kind of the new imidazoline compounds) comprises of: adding triethyl phosphonoacetate 56g(0.25M) solution in tetrahydrofurane(THF) 70ml to NaH 6g(0.25M) suspension in THF 600ml maintained at 0C under nitrogen atmosphere drop by drop; shaking the mixture for 30minutes at 10C, cooling to 0C, and treating with beta-tetralone 36.52g(0.25M) solution in anhydrous THF 50ml drop by drop; shaking for 3hrs at 20C, hydrolyzing the mixture with water 200ml at 0C; distilling the solvent under decompression, and extracting the residue with dichloromethane; washing the gathered organic phase with saturated NaCl solution, drying, and concentrating to get ethyl 2-(3,4-dihydro-naphtyl-2-yl)acetate; gaining the 4-(3,4-dihydro-2-naphtylmethyl)4,5-dihydro-1H-imidazole fumarate from the ethyl 2-(3,4-dihydro-naphtyl-2-yl)acetate.