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Orlistat preparation method

A technology of orlistat and its products, which is applied in the field of drug preparation, can solve the problems of high production cost and complicated manufacturing process, and achieve the effect of low production cost and simple preparation process

Inactive Publication Date: 2015-07-01
李磊
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the current process of producing orlistat, the manufacturing process is complicated and the production cost is high

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0006] Now in conjunction with the present invention for further detailed description.

[0007] A kind of preparation method of orlistat of the present invention, concrete steps are as follows: (3S, 4S)-3-hexyl-4-[(R)-2-hydroxytridecyl]-2-oxetanone , triphenylphosphine and N-formyl-L-leucine were dissolved in tetrahydrofuran, diethyl azodicarboxylate was added dropwise under stirring, and stirring was completed overnight, the organic phase was taken out, concentrated under reduced pressure, and the residue was silica gel Column chromatography yielded the product orlistat.

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PUM

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Abstract

The present invention relates to an orlistat preparation method, which concretely comprises: dissolving (3S, 4S)-3-hexyl-4-[(R)-2-hydroxy tridecyl]-2-oxetanone, triphenyl phosphorous and N-formyl-L-leucine in tetrahydrofuran, adding diethyl azodicarboxylate in a dropwise manner under stirring, stirring overnight, taking out the organic phase, carrying out pressure reducing concentration, and carrying out silica gel column chromatography on the remaining material so as to obtain the product orlistat. The orlistat preparation method of the present invention has characteristics of simple preparation process and low production cost.

Description

technical field [0001] The invention relates to the field of medicine preparation, in particular to a preparation method of orlistat. Background technique [0002] Orlistat is currently the only OTC weight loss drug in the world. More than 40,000,000 people around the world have taken it and successfully lost weight. It is currently the best-selling weight loss product. It is effective for weight loss. Orlistat is a potent and long-acting specific gastrointestinal lipase inhibitor. By directly blocking the body's absorption of fat in food, once the intake of heat and fat is less than consumption, Naturally reduce body fat, so as to achieve the purpose of weight loss. It is safe to lose weight, the active ingredients do not enter the blood circulation, do not act on the central nervous system, have fewer side effects, and will not cause dizziness, palpitation, insomnia, dry mouth, etc. Because it is currently in the process of producing orlistat, the manufacturing process i...

Claims

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Application Information

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IPC IPC(8): C07D305/12
CPCC07D305/12
Inventor 李磊
Owner 李磊