---- 4-- New Synthetic Method for the Intermediate -N-Methyl-4-trifluoromethyl-phenoxy benzenepropane amine.

摘要

PURPOSE: A method for preparing the intermediate for the preparation of ()-N-methyl- -£4-(trifluoromethyl)-phenoxy|benzenepropaneamine(fluoxetine) of the formula 1 with the antidepressant activity is provided, to use a safe and inexpensive starting material and not to use the compressed hydrogen gas, thereby reducing the cost and enhancing the stability. CONSTITUTION: The intermediate is a hydroxyetser compound represented by the formula 5, wherein R and R' is independent each other and are a straight or branched alkyl group of C1-C5. The intermediate is prepared by reacting an aldehyde and a bromoalkylester with Zn. Preferably the intermediate is prepared by reacting benzaldehyde and an alkyl -bromopropionate with Zn in a solvent comprising benzene or toluene with refluxing under the inert condition; and treating the product with an inorganic acid.