Fosaprepitant supercritical reaction preparation method

A fosaprepitant and supercritical technology, applied in the field of supercritical reaction preparation of fosaprepitant, can solve the problems of low efficiency and long operation period, and achieve the effects of accelerating diffusion, accelerating temperature increase and improving preparation efficiency

Inactive Publication Date: 2019-04-12
SICHUAN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The technical problem to be solved by the present invention is: in the existing fosaprepitant supercritical reaction preparation, the efficiency is not high when stirring, the reaction and filtration are carried out separately on different equipment, and the operation period is long

Method used

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  • Fosaprepitant supercritical reaction preparation method
  • Fosaprepitant supercritical reaction preparation method
  • Fosaprepitant supercritical reaction preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] A kind of fosaprepitant supercritical reaction preparation method, comprises the steps:

[0055] Step 1: Turn on the drive motor 5, adjust the rotating speed to 120-150rpm, and the inner tank 3 rotates slowly relative to the outer tank 2;

[0056] Step 2: add aprepitant dibenzyl phosphate and palladium carbon with a mass fraction of 5% in the inner tank 3 through the raw material and catalyst inlet 13 respectively, and the amount of palladium carbon added is aprepitant dibenzyl phosphate 0.5% by weight;

[0057] Step 3: Pass carbon dioxide through the carbon dioxide inlet 10 to replace the air in the tank;

[0058] Step 4: Passing hydrogen gas from the hydrogen gas inlet 11 to form a hydrogen partial pressure of 0.6-0.7 MPa;

[0059] Step five: feed carbon dioxide from the carbon dioxide inlet 10 so that the air pressure in the tank is 13-14MPa;

[0060] Step 6: Turn on the heating element 19 so that the temperature in the tank is 35-36°C;

[0061] Step 7: Adjust th...

Embodiment 2

[0081] The difference between this embodiment and Embodiment 1 is that there are two stirring paddles 7 and the sub-blades 8 facing the inner recess of the arc-shaped structure are respectively arranged at the bottom thereof, and the sub-blades 8 can assist in stirring the raw material at the lower end of the inner recess, so that The raw materials at the upper end of the inner concave part can fall and be turned to achieve more uniform and efficient mixing.

[0082] The stirring shaft 6 is located inside a section of the inner tank 3 and a heating element 19 is provided.

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Abstract

The invention discloses a fosaprepitant supercritical reaction preparation method, and solves the problems of low stirring efficiency, separate reaction and filtration on different equipment, and longoperation period in existing fosaprepitant supercritical reaction preparation. The method includes the steps of: feeding, air replacement, filling of hydrogen and carbon dioxide, heating and stirringfor supercritical reaction, dissolution of the reaction product by a solvent and filtration. The method provided by the invention has the advantages of high stirring efficiency, short preparation period, etc.

Description

technical field [0001] The invention relates to the technical field of fosaprepitant preparation, in particular to a method for preparing fosaprepitant by supercritical reaction. Background technique [0002] Fosaprepitant, also known as Fosaprepitant, is an NK1 receptor antagonist developed by Merck, which mainly acts by blocking the nausea and vomiting signals in the brain. It was approved for marketing by the US FDA in 2008. Its structure is as follows I show. [0003] [0004] In the prior art, the method for preparing fosaprepitant generally carries out catalytic hydrogenation by adding palladium carbon to the raw material, but due to the gas, liquid and solid heterogeneous reactions of catalytic hydrogenation under conventional conditions, the gap between the raw material and the catalyst The contact area is very limited. In order to make the catalytic hydrogenation reaction go completely, generally 5%-20% by weight of precious catalyst palladium carbon will be add...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F9/6558B01J3/00B01J3/04B01J19/00B01J19/28
CPCB01J3/002B01J3/04B01J19/0013B01J19/0053B01J19/0066B01J19/28B01J2219/00076B01J2219/00162C07F9/65583Y02P20/54
Inventor 周逸杰高天睿包莹
Owner SICHUAN PHARMA
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