1448326-33-7Relevant articles and documents
Novel synthesis method of crizotinib intermediate (by machine translation)
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, (2021/01/04)
The invention relates to a synthesis method of an organic compound, in particular to a novel synthesis method of a crizotinib intermediate, which comprises the following steps: taking cheap and easily available 2,6 - dichloro -3 - fluoroacetophenone as a starting raw material and reducing the CBS system to obtain S-shaped chiral alcohol. , 2 - Aminopyridine is taken as a raw material and bromine is brominated to obtain 3,5 - dibromo -2 - aminopyridine. The compound is condensed into an ether with a chiral alcohol under the action of an acid-binding agent to obtain the intermediate of the required configuration. The method is simple in reaction, short in route, less in three wastes, environment-friendly, high in yield of all steps, and less in raw material and reagent waste. (by machine translation)
Novel pyridine derivatives having inhibition activity against SHIP2 and pharmaceutical compositions with the components
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Paragraph 0419; 0435; 0437; 0439; 0440, (2020/03/24)
The present invention relates to a use as a pyridine derivative and/or a SHIP2 inhibitor. More specifically, the present invention relates to: a pyridine derivative of chemical formula I or pharmaceutically acceptable salt thereof; a method for manufacturing compounds thereof; and a pharmaceutical composition containing the compounds as active components. The pyridine derivative and the pharmaceutically acceptable salt thereof are useful as therapeutic agents for diseases related to SHIP2, such as Alzheimerandprime;s dementia, hypertension, cancer, diabetes, etc.COPYRIGHT KIPO 2020
Synthesis of a Crizotinib Intermediate via Highly Efficient Catalytic Hydrogenation in Continuous Flow
Chen, Jianli,Cheng, Pengfei,Su, Weike,Xie, Xiaoxuan,Xu, Feng,Yu, Zhiqun
supporting information, p. 2252 - 2259 (2020/11/26)
Kilogram-scale highly selective catalytic hydrogenation of the aryl nitro group in the intermediate of crizotinib has been developed, which adopted continuous-flow technology with prepassivated Raney Ni as a catalyst at room temperature. According to the reaction condition optimization, side reactions such as dehalogenation, debenzylation, and reduction of other unsaturated functional groups were inhibited eminently. Moreover, catalytic hydrogenation of (R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-2-nitropyridine (compound I) afforded the desired product (R)-3-[1-(2,6-dichloro-3-fluorophenyl)ethoxy]pyridin-2-amine (compound II) with high selectivity (99.9%) and high conversion (99.5%). Finally, high-quality crizotinib was synthesized from intermediate II.