1404234-03-2Relevant articles and documents
Preparation and detection method of dapoxetine hydrochloride isomer impurities
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Paragraph 0013; 0017-0018, (2020/05/01)
The invention discloses a preparation process for preparing a dapoxetine hydrochloride beta-isomer impurity shown as formula I and an enantiomer shown as formula II. The method comprises the following steps: taking optically pure Boc-(S) or (R)-3-amino-3-phenylpropanol as a raw material, performing condensation reaction with 2-fluoronaphthalene or 1-fluoronaphthalene, performing methylation reaction with formic acid-formaldehyde, and performing HCl salification reaction to obtain a target product dapoxetine hydrochloride beta-isomer or enantiomer impurity. Meanwhile, a detection method of isomer impurities is developed.
Preparation method of dapoxetine hydrochloride impurities
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, (2018/06/15)
The invention discloses a preparation method of three impurities with similar structures for dapoxetine hydrochloride: (S)-3-(naphthalene-1-oxo)-1-phenylpropy-1-amine (compound II), (S)-N-methyl-3-(naphthalene-1-oxo)-1-phenylpropy-1-amine (compound III) and (S)-N,N-dimethyl-3-(naphthalene-2-oxo)-1-phenylpropy-1-amine (compound IV). The preparation method comprises the following steps: taking (S)-3-amino-3-phenylpropy-1-ol (VII) as a starting raw material; carrying out a multiple-step reaction such as amino protection, hydroxyl activation, substitution and amino deprotection to respectively obtain a compound II, a compound III and a compound IV as impurities of the dapoxetine hydrochloride. According to a preparation route, the starting raw materials are easy to obtain; reaction conditionsare mild and the selectivity is high; a sample with higher purity (98 percent or above) can be obtained according to a conventional post treatment method, can be used as a reference substance of the compound II, the compound III and the compound IV that are impurities of the dapoxetine hydrochloride and is used for quality control over synthesis research of the dapoxetine hydrochloride.
Midbody for preparing dapoxetine and preparation method for dapoxetine
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Paragraph 0034; 0035, (2018/04/02)
The invention relates to a midbody for preparing dapoxetine and a preparation method for dapoxetine. The dapoxetine hydrochloride with high optical purity can be acquired through a preparation path provided by the invention according to the steps of perfo