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.
Synthesis method of dapoxetine and dapoxetine hydrochloride
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Paragraph 0088; 0096-0099, (2021/10/02)
The invention provides a synthesis method of dapoxetine and dapoxetine hydrochloride, and belongs to the technical field of organic synthesis of medicines. The synthesis method of dapoxetine provided by the invention comprises the following steps: 1-naphthol and paraformaldehyde generate 1-naphthol bromomethyl ether under the action of hydrogen bromide, the 1-naphthol bromomethyl ether reacts with magnesium to obtain a 1-naphthol bromomethyl ether Grignard reagent, the 1-naphthol bromomethyl ether Grignard reagent reacts with R-styrene oxide to obtain R-3-(1-naphthyloxy)-1-phenyl propanol, and the R-3-(1-naphthyloxy)-1-phenyl propanol reacts with a bromination reagent to obtain S-1-bromo-1-phenyl-3-(1-naphthyloxy)propane; or the S-1-bromo-1-phenyl-3-(1-naphthyloxy)propane reacts with sulfonyl chloride to obtain S-1-sulfonyloxy-1-phenyl-3-(1-naphthyloxy) propane, or and the S-1-sulfonyloxy-1-phenyl-3-(1-naphthyloxy)propane reacts with sulfonyl chloride to obtain dapoxetine hydrochloride. The synthesis method provided by the invention has the advantages of short synthesis route, high product yield, good product quality, easily available raw materials, low cost and small environmental pollution, and is suitable for industrial production.
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.