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Refining method of fosaprepitant dimeglumine

A technology of fosaprepitant dimeglumine and its refining method, which is applied in the field of refining fosaprepitant dimeglumine bulk drug, and can solve the problems such as difficult drying of solvents

Inactive Publication Date: 2015-05-27
SHANGHAI HUILUN BIOLOGICAL TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] The solvents used in the above prior art are used as poor solvents. During the scale-up production process, the solvent residues are difficult to dry to meet the residue limit requirements of pharmaceutical regulations.

Method used

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  • Refining method of fosaprepitant dimeglumine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Dissolve 40g of fosaprepitant dimeglumine in 160ml of methanol solution dropwise into 500ml of isopropanol solvent that is being stirred, control the temperature below 20°C, and precipitate a solid, continue stirring for 0.5 to 1 hour after dropping, filter, The filter cake was washed with 50ml of acetone, the filter cake was beaten with 500ml of acetone, stirred for half an hour, filtered, the solid was collected, and vacuum-dried for 8 hours to obtain 37.4g of fosaprepitant dimeglumine with a yield of 93.5%.

Embodiment 2

[0022] Dissolve 25g of fosaprepitant dimeglumine in 100ml of methanol solution into 400ml of isopropanol solvent which is being stirred, and control the temperature at 20°C to precipitate a solid. Continue stirring for 0.5 to 1 hour after dropping, and filter. The filter cake was washed with 20 ml of ether, and the filter cake was slurried with 150 ml of ether, stirred for half an hour, filtered, and the solid was collected and vacuum-dried for 8 hours to obtain 23.8 g of fosaprepitant dimeglumine, with a yield of 95.2%.

Embodiment 3

[0024] Dissolve 25g of fosaprepitant dimeglumine in 100ml of methanol into a stirred 400ml of ethanol / acetonitrile (1:1) solvent, control the temperature at about 20°C, and precipitate a solid, continue stirring for 0.5~ 1 hour, filtered, the filter cake was washed with 20ml of ether, the filter cake was beaten with 150ml of ether, stirred for half an hour, filtered, the solid was collected, and vacuum-dried for 8 hours to obtain 22.3g of fosaprepitant dimeglumine, with a yield of 89.2% .

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Abstract

The invention belongs to the field of chemicals and specifically relates to a refining method of a fosaprepitant dimeglumine crude drug. During refining process, acetone or ether is used to wash a product, and a high-toxicity acetonitrile solvent used in the prior art is replaced. Purity of the obtained fosaprepitant dimeglumine crude drug is high; solvent residue content is low; drying temperature is reduced; and drying time is shortened. The refining method provided by the invention is suitable for industrial production.

Description

technical field [0001] The invention belongs to the field of chemical medicines, and in particular relates to a method for refining fosaprepitant dimeglumine crude drug. Background technique [0002] Fosaprepitant dimeglumine (Fosaprepitant dimeglumine) was developed by Merck, and another drug of the company, Aprepitant (Aprepitant), is clinically used as an adjuvant drug in the treatment of brain tumors to prevent chemotherapy-induced acute and delayed nausea and vomiting. Fosaprepitant and aprepitant belong to the class of neurokinin-1 (NK-1) receptor antagonists or substance P antagonists, which mainly work by blocking the nausea and vomiting signals in the brain. The NK-1 receptor is the binding site for tachykinin (NKA) substance P (SP), located in the brainstem vomiting center and the gastrointestinal tract. Animal experiments have proved that SP can induce vomiting, and drugs that specifically block this receptor can prevent vomiting caused by all emetogenic stimuli...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F9/6558C07C215/10C07C213/10
Inventor 秦继红
Owner SHANGHAI HUILUN BIOLOGICAL TECH CO LTD
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