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Preparation process of HER2 small-molecule inhibitor Fikatinib

A preparation process and mixed solvent technology are applied in the field of preparation technology of HER2 small molecule inhibitor tucatinib, which can solve the problem that the preparation process of tucatinib needs to be improved.

Active Publication Date: 2022-04-01
武汉九州钰民医药科技有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005]However, the preparation process for tucatinib still needs to be improved

Method used

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  • Preparation process of HER2 small-molecule inhibitor Fikatinib
  • Preparation process of HER2 small-molecule inhibitor Fikatinib
  • Preparation process of HER2 small-molecule inhibitor Fikatinib

Examples

Experimental program
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Embodiment 13

[0075] Embodiment 13 is a comparative example. In this embodiment, the inventor adjusted the compound shown in formula 3, K 2 CO 3 , the molar ratio of the compound shown in formula 8 is 1:1.6:1.5, and the compound shown in the adjustment formula 3, K 2 CO 3 , The reaction time for the compound shown in formula 8 to contact and stir is 3h. The result shows that embodiment 13 is technically effective, compared to the compound shown in formula 3 described in embodiment 10~embodiment 12 of the present invention, K 2 CO 3 , the final product obtained when the mol ratio of the compound shown in formula 8 is 1:(1~1.3):(1~1.2), the purity of the product that obtains through embodiment 13 will reduce, and impurity increases, and embodiment 13 has caused The actual waste of reactant raw materials, the yield of the target compound obtained has not been improved.

[0076] At room temperature, compound (24.03g, 100mmol) shown in formula 3 and K 2 CO 3 (22.11g, 160mmol) was added to...

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Abstract

The invention provides a preparation process of an HER2 small-molecule inhibitor graphic-batatinib. Compared with the prior art, in the step (1), the compound shown in the formula 1, the compound shown in the formula 2, triphenylphosphine and diethyl azodicarboxylate are contacted, a Mitsunobu reaction is adopted, phenolic hydroxyl groups can be specifically reacted, the reaction site is single, the defect that heating is needed in the halogenation reaction can be avoided, and the method has the advantages of being mild in condition, high in yield and the like. And the operation is simple. The synthetic route and the preparation process have the advantages of short steps, mild conditions and easiness in operation, and can be suitable for the operability of industrial mass production.

Description

technical field [0001] The invention relates to the technical field of biomedicine, in particular to a preparation process of tucatinib, a small molecule inhibitor of HER2. Background technique [0002] Tucatinib (R&D code ARRY-380, ONT-380, trade name Tukysa) is a small molecule oral tyrosine kinase inhibitor with excellent targeting selectivity for HER2. On April 18, 2020, the US FDA approved the listing of Tucatinib, a selective HER2 inhibitor developed by Seattle Genetics, which is used in combination with trastuzumab and capecitabine for the treatment of surgical Adult patients with unresectable or metastatic advanced HER2-positive breast cancer. [0003] The chemical structure of tucatinib is shown in formula I: [0004] [0005] However, the current preparation process for tucatinib still needs to be improved. Contents of the invention [0006] The present invention aims to solve one of the technical problems in the related art at least to a certain extent. T...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D471/04
Inventor 范昭泽黄祥泉余艳平胡仁军
Owner 武汉九州钰民医药科技有限公司
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