Process Research Of Citalopram Hydrobromide

Citalopram Hydrobromide is one of the new generation anti-depressants. Its side effects are rather small, allergic reactions seldom to happen, using to treat major depression, and being easy to take.With comprehensive study on local and overseas literatures, we have selected a synthesis route which fits for industrial production. With plenty of repeated experiments, I have successfully improved the feasibility of each step.Pertain to Grignard reaction, THF was distilled directly after the reaction so as to solve the problem of high water content of recycling THF, thus reduced its consumption. In the reduction , LiAlH4 was replaced by KBH4,and reduced the quantity of KBH4. choose ethanol to replace THF to accelerate the reaction and make the reduction more completed.In the late stage treatment to Cyanogenation, The target compound was distilled directly, and avoid washing the product by the very toxic NaCN solution.Finally, to further reduce the production cost and simplified the operation procedure we have combined the first three steps together without separating and purifying the intermediate of each step. The yield of Citalopram Hydrobromide is 40.12% after our optimization, 22.86% higher than patent yield.We have qualified the analytical method according to'The People's Republic of China Pharmacopoeia 2005 edition'and'United States Pharmacopoeia 30th edition'respectively.