Improved synthesis of dapoxetine hydrochloride
Abstract
For the shortcomings and deficiencies of synthesis of dapoxetine hydrochloride,the method was optimized and improved.It started from 3-phenylpropanol,which underwent etherification with 1-fluoronaphthalene in the presence of sodium hydride,followed by bromination by NBS using AIBN as catalyst,substitution with dimethyl amine,resolution by L-(+)-tartaric acid to give dapoxetine free base and formation of dapoxetine hydrochloride with an overall yield of 21.0%.This improved process reduced the use of expensive raw materials and toxic reagents with relatively convenient operation procedure and was more suitable for large-scale industrial production.
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