Refining method of fosaprepitant dimeglumine

A fosaprepitant dimeglumine and refining method technology, applied in the field of medicine, can solve the problems of high drying temperature, easy degradation, long drying time, etc., and achieve the effect of reducing degradation and low solvent residue

Active Publication Date: 2013-01-02
JIANGSU AOSAIKANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] In the above prior art, it is necessary to use some alcohol or ketone solvents as anti-solvents. During the vacuum drying process, it is difficult to dry the residues of alcohol or ketone solvents to meet the residue limit requirements of drug regulations.
In order to meet the requirements of the drug solvent residue limit of the regulations, a longer drying time and a higher drying temperature are required, and in a longer drying time, fosaprepitant dimeglumine is easily degraded

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Dissolve 50 g of the crude product of fosaprepitant dimeglumine in 100 ml of methanol. With stirring, add the methanol solution dropwise to 498 ml of acetonitrile to precipitate a solid. After the addition is complete and stir for 30 minutes, filter under nitrogen protection. After vacuum drying at ℃ for 14 hours, 43.6 g of the finished product of fosaprepitant dimeglumine was obtained, with a yield of 87.20%.

[0030]

Embodiment 2

[0032] Dissolve 42.5 g of the crude product of fosaprepitant dimeglumine in 85 ml of methanol. With stirring, add the methanol solution dropwise to 423 ml of acetonitrile to precipitate a solid. After the addition is complete and stir for 30 minutes, filter under nitrogen protection. Vacuum drying at 35°C for 10 hours yielded 36.3 g of the finished fosaprepitant dimeglumine, with a yield of 85.30%.

[0033]

Embodiment 3

[0035] Dissolve 87.6g of the crude product of fosaprepitant dimeglumine in 218ml of methanol. With stirring, add the methanol solution dropwise to 654ml of acetonitrile to precipitate a solid. After the addition is complete and stir for 30 minutes, filter under nitrogen protection. After vacuum drying at 38°C for 8 hours, 73.8 g of the finished fosaprepitant dimeglumine was obtained, with a yield of 84.20%.

[0036]

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PUM

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Abstract

The invention belongs to the field of medicine and relates to a refining method of fosaprepitant dimeglumine. In a refining process, single acetonitrile is used as an anti-solvent for carrying out crystallization treatment on products, and a mixed solvent used in the prior art is replaced. The purity of the obtained fosaprepitant dimeglumine raw material medicine is high, the solvent residue amount is fewer, particularly, the temperature and vacuum degree requirements in a drying process are low, and the refining method is suitable for industrial production.

Description

[0001] technical field [0002] The invention belongs to the field of medicine, and relates to a preparation method of fosaprepitant dimeglumine, more specifically to a refining method of fosaprepitant dimeglumine. [0003] Background technique [0004] Fosaprepitant, also known as fosaprepitant, is the prodrug of aprepitant, which is rapidly converted into aprepitant in the body after injection. In 2008, fosaprepitant dimeglumine was approved by the FDA for marketing. Fosaprepitant and aprepitant are human substance P / neurokinin 1 (NK-1) selective high-affinity receptor blockers, which mainly function by blocking the brain's nausea and vomiting signals. Fosaprepitant dimeglumine is clinically used as an adjuvant drug for tumor treatment to prevent acute and delayed nausea and vomiting caused by chemotherapy. [0005] In the current open literature, there are two synthetic methods for fosaprepitant dimeglumine: one is to hydrogenate aprepitant dibenzyl phosphate, and then ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F9/6558C07C215/10C07C213/10
Inventor 赵俊伏世建刘同根
Owner JIANGSU AOSAIKANG PHARMA CO LTD
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