Citalopram Intermediates Synthesized

Citalopram is a well know antidepressant drug that has now been on market for tens years. It is selective, centrally acting serotonin (5-hydroxytryptamine) reuptake inhibitor, accordingly having well antidepressant activities; the side effect is very limited. The compound has further been disclosed to show effects in the treatment of dementia and cerebrovascular disorders.There are many methods for manufacture of the Citalopram. Two easy and convenient method for synthesizing citalopram are selected in this paper .The major purpose of this paper is engaged in research about preparation for two intermediates-5-cyanothphalide and 5-aminophthalimide, using as the starting material for synthesis of citalopram, especially searching a new methods of preparation for these intermediates (The methods of preparation for them have been applied to our country for patents.). The application of these discovers to industry has been realized.5-cyanophthalide is synthesized through two steps: (1) the 5-carbonphthalide is used as starting material. It is aminated with concentrated ammonia spirit. (2) 5-ammonium formate phthalide is reacted with dehydrating agent. By the process of this invent, 5-cyanophthalide is obtained in a high yield (above 82%), cost-effective way and by a convenient process. The product possesses high quality, and the pollution to environment is reduced.5-aminophthalimide is prepared by reduction of 5-nitrophthalimide using as starting material. Many experiments have been finished for looking for an adequate reducing agent and searching a quality solvent. The by-product Fe powder of machining and dimethyl suloxide is selected as reducing agent and solvent, by the end. By theprocess of this paper ,5-aminophthalimide is obtained in a high yield (above 89%), cost-effective way and by a convenient process. The product possesses high quality, and the pollution to environment is reduced.Two intermediates have been produced in our factory and grown good benefit.