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Preparation method of tomoxetine medicine

A technology of atomoxetine and medicine, which is applied in the field of preparation of atomoxetine medicine, and achieves the effect of simple procedure, high efficiency and short preparation process time

Inactive Publication Date: 2015-06-03
葫芦岛国帝药业有限责任公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The method solves the technical problem of atomoxetine preparation by mixing a strong base with N-methyl-3-hydroxyl-3-phenylpropylamine, and then adding o-fluorotoluene dropwise

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] 20 g of 0.121 mol of N-methyl-3-hydroxy-3-phenylpropylamine and 22.6 g of 0.565 mol of sodium hydroxide were mixed and heated to 80°C, stirred to form a slurry, heated to 100°C, and maintained for 2 hours. 40 g of 0.363 mol o-fluorotoluene was added dropwise to the resulting slurry. Heat the mixture to 100°C and keep it for 3 hours, then add 200ml of water and cool to room temperature, add ethyl acetate for extraction, separate layers, back extract the aqueous layer with ethyl acetate, collect the organic phase and wash twice with water. Concentrate to obtain 27.8 grams of atomoxetine. Yield: 90.0%.

Embodiment 2

[0017] 20 g of 0.121 mol N-methyl-3-hydroxy-3-phenylpropylamine and 34 g of 0.606 mol potassium hydroxide were mixed and heated to 0.606 mol, stirred to form a slurry, heated to 100° C., and maintained for 2 hours. The resulting slurry was added dropwise with 40 g of 0.363 mol o-fluorotoluene. Heat the mixture to 100°C and keep it for 3 hours, add 200ml of water and cool to room temperature, add ethyl acetate for extraction, separate layers, back-extract the aqueous layer with ethyl acetate, collect the organic phase and wash twice with water. Concentration gave 30.3 g of atomoxetine. Yield: 98.1%.

Embodiment 3

[0019] 20 g of 0.121 mol of N-methyl-3-hydroxy-3-phenylpropylamine and 13.0 g of 0.242 mol of solid sodium methoxide were mixed and heated to 60°C, stirred to form a slurry, heated to 60°C, and maintained for 1 hour. The resulting slurry was added dropwise with 40 g of 0.363 mol o-fluorotoluene. Heat the mixture to 80°C and keep it for 4 hours, add 200ml of water and cool to room temperature, add ethyl acetate for extraction, separate layers, back-extract the aqueous layer with ethyl acetate, collect the organic phase and wash twice with water. Concentrate to obtain 25.6 grams of atomoxetine.

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PUM

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Abstract

The invention provides a preparation method of tomoxetine medicine, which comprises the steps of: heating alkali and N-methyl-3-hydroxyl-3-phenylpropylamine to form a mixture, adding o-fluorotoluene into the mixture to form another mixture, and heating the mixture to obtain the tomoxetine. The method is simple in process, short in time of the preparation process and high in efficiency. The method is suitable for being applied to preparation of the tomoxetine medicine.

Description

technical field [0001] The invention proposes a pharmaceutical method in the pharmaceutical field, specifically a method for preparing atomoxetine. Background technique [0002] Tomoxetine, Chinese chemical name: N-methyl-3-(2-methylphenoxy)-3-phenylpropylamine, atomoxetine is an important intermediate of atomoxetine hydrochloride, tromoxetine hydrochloride Moxetine is mainly used to treat attention deficit and hyperactivity disorder. [0003] There have been several methods in the prior art to prepare atomoxetine, such as: US4018895 reported that 3-bromo-1-phenylpropanyl chloride and o-cresol are formed into ethers, and then monomethylamine is aminated to prepare Atomoxetine approach. [0004] US6541668 has reported the synthesis of atomoxetine, with potassium tert-butoxide, solvent selection 1,3-dimethyl-2-imidazolinone or N-methylpyrrolidone, the price is more expensive, the reaction temperature is high and the time is long 12 -48 hours, lower yield. [0005] In Tetra...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C217/48C07C213/06
Inventor 张忠义汪家勇张厦
Owner 葫芦岛国帝药业有限责任公司
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