70398-95-7Relevant articles and documents
Ceritinib intermediate and method for preparing ceritinib
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Paragraph 0112; 0113, (2019/05/28)
The invention relates to a ceritinib intermediate and a method for preparing ceritinib. A ceritinib intermediate compound is 4-isopropoxy-5-guanidyl-2-N-substituted piperidine-4-base toluene nitrate (VII). The method includes carrying out substation reaction on 2-nitro-4,5-dimethyl chlorobenzene and isopropyl alcohol in the presence of alkali to generate compounds III; carrying out condensation onthe compounds III and halogenated acetaldehyde di-acetal and carrying out reduction ring formation by ammonia-ammonium chloride-sodium borohydride to obtain compounds IV; carrying out amino protection to obtain compounds V; carrying out catalytic hydrogenation in solvents and carrying out nitro reduction to obtain amino so as to obtain compounds VI; carrying out reaction on the compounds VI and cyanamide to obtain compounds VII. The ceritinib can be prepared from the compounds VII by the aid of the method. The ceritinib intermediate and the method have the advantages of inexpensive and easilyavailable raw materials, simplicity and convenience in operation, high elementary reaction selectivity, low wastewater quantity and green environmental protection.
