1071929-03-7Relevant articles and documents
Synthesis method of dapoxetine
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Paragraph 0040; 0047-0049; 0051; 0057-0058; 0061-0063, (2022/01/12)
The present invention provides a synthesis method of dapoxetine, comprising the following steps: S1, the (s)-3-amino-3-phenylpropionic acid or ester compounds dispersed in a solvent, reflux reaction under the action of a reducing agent, to give (s) - amino-3-phenylpropanol; S2, the (s) - amino-3-phenylpropanol dissolved in aqueous solution of carboxylic acid, added paraformaldehyde to warm up the reaction, to give (s) -3-dimethylamino-3-phenylpropanol; S3, (s)-3-Dimethylamino-3-phenylpropanol was dissolved in a solvent, protected by nitrogen, and reacted in a solution of alkali added dropwise at a higher temperature, and then 1-fluoronaphthalene was added to produce Williamson etherization reaction, to give (s)-N, N-dimethyl-3-(1-naphthooxy) amphetamine, i.e., dapoxetine. The synthesis method of dapoxetine of the present invention is inexpensive and easy to obtain raw materials, does not use toxic and dangerous reagents, will not react to the phenomenon of aggregation spray, the process is simple, suitable for industrial production.
Resolution method of dapoxetine
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Paragraph 0013-0016, (2021/01/11)
The invention relates to a chemical resolution method of dapoxetine, and belongs to the technical field of drug synthesis. Specifically, (+)-camphor-10-sulfonic acid is used as a resolution reagent, and optically pure dapoxetine hydrochloride is obtained by salifying, crystallizing, separating, alkalizing, salifying and the like. The preparation method of optically active (S)-(+)-dapoxetine hydrochloride is simple and convenient to operate, low in cost and high in purity.
Related substances of dapoxetine hydrochloride, preparation method and applications thereof
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, (2020/04/17)
The invention relates to related substances of dapoxetine hydrochloride, a preparation method and applications thereof, wherein the related substances are (R)-3-((R)-3-(naphthalene-1-oxy)-1-phenylpropoxy)-1-phenylpropyl-1-ol and/or (S)-N,N-dimethyl-3-((R)-3-(naphthalene-1-oxy)-1-phenylpropoxy)-1-phenylpropyl-1-amine and a salt thereof, especially a hydrochloride. According to the invention, by detecting and controlling the related substances provided by the invention in the production and quality inspection of dapoxetine hydrochloride, an intermediate, a bulk drug and a preparations thereof, the drug quality of dapoxetine hydrochloride is further improved, possible side effects are reduced, and the medication safety is improved.