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Method for preparing duloxetine

A technology of duloxetine and thienyl group, applied in the field of preparation of duloxetine

Inactive Publication Date: 2009-03-25
SUZHOU LEADER CHEM
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

But the total yield of duloxetine of this method only reaches 19% at the highest

Method used

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  • Method for preparing duloxetine
  • Method for preparing duloxetine
  • Method for preparing duloxetine

Examples

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Embodiment Construction

[0021] The following are specific examples of the present invention to further describe the technical solution of the present invention, but the present invention is not limited to the examples.

[0022] Duloxetine according to the present embodiment is prepared according to the following steps:

[0023] (1), Mannich reaction prepares 3-dimethylamino-1-(2-thienyl)-1-acetone hydrochloride, and the equation is as follows:

[0024]

[0025] Set up a device with mechanical stirring, put 100g of 2-acetylthiophene, 37.7g of paraformaldehyde, 91g of dimethylamine hydrochloride and 523ml of ethanol into the three-necked reaction flask in turn, start stirring, and gradually add 3.8ml of concentrated hydrochloric acid dropwise, After dripping, start the water bath to control the temperature to 83°C to reflux. After all the solids were dissolved, reflux was started, and a white solid was formed after 1 hour (at this time, attention should be paid to slowing down the stirring speed), ...

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Abstract

The invention relates to a preparation method of duloxetine, which takes 2-acetyl phenol, paraformaldehyde and dimethylamine hydrochloride as raw materials to obtain the target product by five steps of Mannich reaction, reduction, resolution, etherification and demethylation, and optimizes the reaction conditions of resolution and etherification, wherein, the resolution reaction comprises the steps of one-time resolution, racemization-resolution and secondary racemization-resolution. The invention can improve the yield of the duloxetine and reduce the production cost, and is easy for industrial production.

Description

technical field [0001] The invention belongs to the field of organic chemistry and medicinal chemistry, in particular to a preparation method of duloxetine. Background technique [0002] Duloxetine (Duloxetine), the chemical name is (S)-N-methylamino-3-(1-naphthyloxy)-3-(2-thienyl)-1-propanamine, is a new type of anti Depressants. Since Lilly developed the drug, practitioners have done a lot of research on its synthesis process. [0003] At present, the relatively economical and feasible synthetic route of duloxetine was reported by Guo Lina of Central China Normal University in her master's thesis in 2007. The synthetic route is: starting with 2-acetylphenol, paraformaldehyde, and dimethylamine hydrochloride The target product was obtained through five steps of Mannich reaction, reduction, resolution, ether formation and demethylation. In this paper, the intermediate R-3-N, N-dimethyl-3-1-(2-thienyl)-1-propanol was successfully racemized, and through the racemization-res...

Claims

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Application Information

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IPC IPC(8): C07D333/20A61P25/24
Inventor 郑丽玲毛卢吉宋桃菊宗顺麟许伟
Owner SUZHOU LEADER CHEM
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