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Method for synthesizing crisaborole intermediate by using microchannel reactor

A technology of microchannel reactors and channel reactors, applied in chemical instruments and methods, chemical/physical/physical chemical reactors, compounds containing elements of Group 3/13 of the periodic table, etc., to achieve increased purity and yield, The effect of reducing the content of impurities and improving safety

Inactive Publication Date: 2021-05-07
HEFEI LIFEON PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] Aiming at the deficiencies of the prior art, the present invention provides a method for synthesizing crisborole intermediates using a microchannel reactor, which solves the problems faced by traditional reactors when using butyllithium to synthesize crisborole

Method used

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  • Method for synthesizing crisaborole intermediate by using microchannel reactor
  • Method for synthesizing crisaborole intermediate by using microchannel reactor
  • Method for synthesizing crisaborole intermediate by using microchannel reactor

Examples

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Effect test

Embodiment 1

[0041] A method for synthesizing a crisborole intermediate using a microchannel reactor, specifically comprising the following steps:

[0042] Step 1, dissolving the intermediate a in the organic solution b, mixing evenly, as the material 1, transporting the material 1 to the pre-cooling module in the microchannel reactor through the plunger pump for mixing and pre-cooling;

[0043] Step 2, the reaction alkali solution is used as material 2, and the material 2 is transported to the precooling module in the microchannel reactor by a plunger pump for mixing and precooling;

[0044]Step 3, the precooled material 1 and material 2 in the step 1 and step 2 are delivered to the reaction module group of the microchannel reactor for reaction, and the material 3 is obtained;

[0045] Step 4, dissolving the boric acid ester in the organic solvent c, mixing evenly, as the material 4, transporting the material 4 to the pre-cooling module in the microchannel reactor through the plunger pump...

Embodiment 2

[0058] A method for synthesizing a crisborole intermediate using a microchannel reactor, specifically comprising the following steps:

[0059] Step 1, dissolving the intermediate a in the organic solution b, mixing evenly, as the material 1, transporting the material 1 to the pre-cooling module in the microchannel reactor through the plunger pump for mixing and pre-cooling;

[0060] Step 2, the reaction alkali solution is used as material 2, and the material 2 is transported to the precooling module in the microchannel reactor by a plunger pump for mixing and precooling;

[0061] Step 3, the precooled material 1 and material 2 in the step 1 and step 2 are delivered to the reaction module group of the microchannel reactor for reaction, and the material 3 is obtained;

[0062] Step 4, dissolving the boric acid ester in the organic solvent c, mixing evenly, as the material 4, transporting the material 4 to the pre-cooling module in the microchannel reactor through the plunger pum...

Embodiment 3

[0075] A method for synthesizing a crisborole intermediate using a microchannel reactor, specifically comprising the following steps:

[0076] Step 1, dissolving the intermediate a in the organic solution b, mixing evenly, as the material 1, transporting the material 1 to the pre-cooling module in the microchannel reactor through the plunger pump for mixing and pre-cooling;

[0077] Step 2, the reaction alkali solution is used as material 2, and the material 2 is transported to the precooling module in the microchannel reactor by a plunger pump for mixing and precooling;

[0078] Step 3, the precooled material 1 and material 2 in the step 1 and step 2 are delivered to the reaction module group of the microchannel reactor for reaction, and the material 3 is obtained;

[0079] Step 4, dissolving the boric acid ester in the organic solvent c, mixing evenly, as the material 4, transporting the material 4 to the pre-cooling module in the microchannel reactor through the plunger pum...

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Abstract

The invention discloses a method for synthesizing a crisaborole intermediate by using a microchannel reactor. The method comprises the following steps: dissolving an intermediate a in an organic solution b, uniformly mixing to obtain a material 1, and conveying the material 1 to a pre-cooling module in the microchannel reactor through a plunger pump for mixing and pre-cooling. According to the present invention, the crisaborole intermediate is synthesized by using the microchannel reactor, the continuous online mixing, pre-cooling and reaction of the reaction material liquid can be achieved due to the unique microstructure design of the microchannel reactor, and the mixing reaction can be completed in the short time even if the two-phase or the three-phase is not dissolved, compared with the traditional stirring hydrogenation reaction kettle, the mixing efficiency is improved by more than 100 times, the whole reaction time can be shortened from several hours to about 30 seconds, the impurity content of the product can be greatly reduced due to overhigh local concentration in the process, the purity and the yield of the product are improved, and the safety is also greatly improved.

Description

technical field [0001] The invention relates to the technical field of drug synthesis, in particular to a method for synthesizing a crisborole intermediate using a microchannel reactor. Background technique [0002] Crisaborole, trade name Eucrisa, chemical name 5-(4-cyanophenoxy)-1,3-dihydro-1-hydroxy-2,1-benzoxaborine pentadiene. [0003] Criborole is a phosphodiesterase 4 (PDE4) inhibitor. At present, there are few preparation methods for crisaborole. Among them, the world patent WO2007095638 (Chinese patent CN101420854 of the same family) applied by the original research company Anacor is a compound patent, and Two preparation methods are reported. [0004] Method 1: Synthetic route such as figure 2 , the method uses 2-bromo-5-hydroxybenzaldehyde as a raw material; a protection and deprotection strategy is adopted, that is, the hydroxyl group of benzyl alcohol is protected with chloromethyl methyl ether (MOM-C1), and the protection is removed after the introduction of...

Claims

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Application Information

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IPC IPC(8): C07F5/02B01J19/00
CPCC07F5/02B01J19/0093Y02P20/55
Inventor 季俊虬陈军王猛颜瑞
Owner HEFEI LIFEON PHARMA
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