abstract |
The invention relates to the diol intermediate of citalopram useful for treatment of depression, that is to say, the crystal of free alkali of 3-hydroxymethyl-4-[1-(4Âfluorophenyl)-1-hydrorybutyl-4-(dimethylamino)] butylbenzonitrile, and the method of crystallization thereof. The invention has disclosed the method to prepare the pure citalopram, it's purified salts, the optical resolution method of citalopram diol intermediate, the method to prepare SÂcitalopram and it's purified salts by crystals mentioned above. The invention has also disclosed citalopram and it's purified salts, S-citalopram and it's purified salts, as well as pharmaceutical formulation thereof obtained. Using methods of the invention, the quality and yield of the product can be signally improved, and production cost of the medicinal material can be decreased. |