Hai Li
2012
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Journal
Central South Pharmacy
Abstract
Objective To optimize the synthesis of O-desmethylvenlafaxine.Methods The 2-(4-hydroxyphenyl) acetic acid was used as starting material,which was etherified by benzyl bromide via etherification reaction.O-desmethylvenlafaxine succinate was synthesized by amidation,condensation,reduction,hydrolysis,and salt formation reaction.Results The synthetic process avoided using dimethylamine,n-butyllithium,and lithium aluminum hydride.The total yield was 30%.Conclusion The synthetic route is simple and economic.The reaction condition is mild and suitable for industrial production.The structure of O-desmethylvenlafaxine succinate is elucidated by 1H-NMR and MS.