1035230-24-0Relevant articles and documents
Preparation method and application of ceritinib intermediate
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Paragraph 0038-0041, (2019/05/04)
The invention relates to a preparation method and application of a ceritinib intermediate, in particular to a preparation process of an intermediate which is 2,5-dichloro-N-(2-(isopropylsulfonyl) phenyl)pyrimidine-4-amine, and belongs to the field of medicine synthesis. The preparation method includes the detailed following steps that a compound 1-a, a compound 1-b, palladium acetate, 9,9-dimethyl-4,5-bis(diphenylphosphino)xanthene and alkali are added into a solvent, a reaction is conducted, and then the ceritinib intermediate can be prepared. The route is simple and short, operation is easy,production costs are lowered, and the preparation method is suitable for large-scale industrialized production.
ALK KINASE INHIBITOR, AND PREPARATION METHOD AND USE THEREOF
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Paragraph 0219; 0220; 0221, (2017/04/18)
An ALK kinase inhibitor compound as represented by Formula I, pharmaceutical composition containing the compound, and preparation method and use thereof in the preparation of drugs serving as an ALK inhibitor for treating cancer.
Ceritinib synthesis intermediate and preparation method thereof
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, (2016/10/10)
The invention provides a synthesis intermediate 8 of an anti-tumor drug ceritinib, a preparation method thereof, and an application of the intermediate 8 in synthesizing ceritinib. The preparation method of the intermediate 8 comprises the following steps: step (1), a compound 1 and an acid HX are subjected to salt formation, such that a compound 7 is obtained; step (2), the compound 7 is reduced through sodium borohydride, such that the compound 8 is obtained. The reaction formula is as the following. With prior arts, expensive platinum oxide is needed as a hydrogenation catalyst for preparing an intermediate 2 in a next step. With the intermediate 8, the above problem is avoided. Therefore, the intermediate 8 is suitable to be used in industrialized production of ceritinib.