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.
A preparation method of the midbody color Switzerland for Nepal
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, (2017/08/24)
The invention relates to a preparation method of ceritinib. The preparation method comprises the following steps: (1) reacting metal powder with N-t-butyloxycarboryl-4 iodine piperidine with a structural formula of SR-1 to generate a metal coupling agent with a structural formula of SR-2; (2) performing a coupling reaction on the metal coupling agent SR-2 and 1-bromo-5-isopropoxy-2-methyl-4-nitrobenzene to generate a compound SR-3; (3) performing hydrogenation reduction on the compound SR-3, and removing BOC amino protection to generate the ceritinib SR-4. According to the invention, a novel preparation method of the ceritinib is developed. The synthetic route is very short; the yield is high; raw materials can be easily obtained and are low in cost; reaction conditions are very mild and easy to control; therefore, the preparation method is suitable for large-scale industrial production.
Ceritinib intermediate and preparation method and application thereof
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Paragraph 0201-0204, (2017/02/28)
The present invention discloses a ceritinib intermediate and a preparation method and application thereof. The ceritinib intermediate has a structure shown as a formula I, R and R2 are as defined in the specification and claims. The ceritinib intermediate is prepared from a compound of a formula 1 and a benzyl halide compound by substitution reaction and then reduction. After further reduction of the nitro by catalytic hydrogenation and removal of amino-protection, the compound of the formula I is reacted with a compound of a formula III to obtain ceritinib. According to the method, raw materials are readily available and inexpensive, the method does not require special equipment, production cost is greatly reduced, and the method is suitable for industrial application.