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Preparation method of dapoxetine hydrochloride free alkali

A compound and oily technology, which is applied in the field of preparation of dapoxetine hydrochloride free base, can solve the problems of poor stability of liquid products, unfavorable development of solid preparations and unfavorable storage of liquid free base, and achieve high yield, convenient mass production, The effect of good practical value

Inactive Publication Date: 2019-03-01
扬子江药业集团江苏紫龙药业有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is only a dosage form of tablets in the market of dapoxetine hydrochloride at present, and for the development of its new dosage form, the research of its main component dapoxetine hydrochloride free base is less
Chinese patent CN103373931 discloses a preparation method of dapoxetine hydrochloride free base, but the free base obtained by it is all oily, compared with solid free base, the stability of liquid is relatively poor, which is not conducive to storage, further industrial production Purification is also relatively difficult, and the liquid free base is not conducive to the development of other solid preparations, such as sublingual tablets, etc.

Method used

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  • Preparation method of dapoxetine hydrochloride free alkali
  • Preparation method of dapoxetine hydrochloride free alkali
  • Preparation method of dapoxetine hydrochloride free alkali

Examples

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preparation example Construction

[0021] The present invention includes a preparation method of the compound of formula I, wherein the preparation is an improvement over the synthesis method of the existing patented dapoxetine hydrochloride free base I.

[0022] definition:

[0023] As used herein, the term "contacting" refers to bringing two or more chemical molecules into proximity so that the two or more chemical molecules react. For example, partially or completely dissolving two or more chemical molecules in one or more solvent systems, mixing one or more chemical substances in a solvent with another or more solid or gas phase chemical substances, etc. Other methods generally known to those skilled in the art.

[0024] As used herein, the term "reaction conditions" refers to the specific circumstances under which a chemical reaction takes place. Including (but not limited to) one or more of the following factors: temperature, solvent, pH, pressure, reaction time, mole ratio of reactants, catalyst, etc. ...

Embodiment 1

[0056] The first step: the compound of formula A and the compound of formula B generate the compound of formula C

[0057] In a 250mL three-necked round-bottomed flask equipped with a magnetic stirrer, add 20ml of methyl tert-butyl ether, add 20mmol of compound A, 40mmol of triethylamine in turn, start stirring, control the temperature at 5-15°C, keep stirring until dissolved After clearing, add 22 mmol methanesulfonyl chloride dropwise, stir for 1 h, and take a sample. TLC detects that the reaction of compound A is basically complete, and the temperature is controlled at 5-15°C for the next step of reaction.

[0058] The second step: the compound of formula C and the compound of formula D generate the compound of formula I

[0059] In the round-bottomed flask in the first step, the temperature was controlled at 5-15 ° C, and 140 mmol of compound D in 2M dimethylamine tetrahydrofuran solution was added, and the temperature was raised to 35 ° C, and stirred until the reaction o...

Embodiment 2

[0068] The first step: the compound of formula A and the compound of formula B generate the compound of formula C

[0069] In a 250mL three-necked round-bottomed flask equipped with a magnetic stirrer, add 20ml of methyl tert-butyl ether, add 20mmol of compound A, 40mmol of triethylamine in turn, start stirring, control the temperature at 5-15°C, keep stirring until dissolved After clearing, add 22 mmol methanesulfonyl chloride dropwise, stir for 1 h, and take a sample. TLC detects that the reaction of compound A is basically complete, and the temperature is controlled at 5-15°C for the next step of reaction.

[0070] The second step: the compound of formula C and the compound of formula D generate the compound of formula I

[0071] In the round-bottomed flask in the first step, the temperature was controlled at 5-15 ° C, and 140 mmol of compound D in 2M dimethylamine tetrahydrofuran solution was added, and the temperature was raised to 35 ° C, and stirred until the reaction o...

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Abstract

The invention discloses a preparation method of dapoxetine hydrochloride free alkali. Solid dapoxetine hydrochloride free alkali can be prepared successfully with the method, yield is high, mass production is facilitated, and the method has greater significance in development of novel dosage forms.

Description

technical field [0001] The invention relates to the fields of medicinal chemistry and organic synthesis, in particular to a preparation method of dapoxetine hydrochloride free base. Background technique [0002] Dapoxetine Hydrochloride (Dapoxetine Hydrochloride), is a selective serotonin reuptake inhibitor (SSRI), developed by Eli Lilly (Eli Lilly) and first listed in Europe in 2009, the trade name is Priligy , has a significant effect in the treatment of premature ejaculation (PE) in men, and this drug is the first oral prescription drug approved for the treatment of PE in the world. However, there is only a dosage form of tablets in the market of dapoxetine hydrochloride at present, and for the development of its new dosage form, the research of its main component dapoxetine hydrochloride free base is less. Chinese patent CN103373931 discloses a preparation method of dapoxetine hydrochloride free base, but the free base obtained by it is all oily matter, compared with so...

Claims

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Application Information

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IPC IPC(8): C07C217/48C07C213/08C07C213/10C07C213/02C07C303/28C07C309/66
CPCC07C213/02C07C213/08C07C213/10C07C303/28C07C309/66C07C217/48
Inventor 戴志成潘瀛鹏钱琴
Owner 扬子江药业集团江苏紫龙药业有限公司
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