796848-79-8Relevant articles and documents
UREA-SUBSTITUTED AROMATIC RING-LINKED DIOXANE-QUINAZOLINE AND -LINKED DIOXANE-QUINOLINE COMPOUNDS, PREPARATION METHOD THEREFOR AND USE THEREOF
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Paragraph 0090-0091, (2020/01/22)
The present invention relates to a urea-substituted aromatic ring-linked dioxane-quinazoline compound of Formula (I) and a urea-substituted aromatic ring-linked dioxane-quinoline, or a pharmaceutically acceptable salt thereof or a hydrate thereof. Also provided are the preparation of the compound as shown in Formula (I) and the pharmaceutically acceptable salt thereof and the use thereof as a drug. The drug is used as an inhibitor of tyrosine kinases (e.g., VEGFR-2, C-RAF, B-RAF) for treating tyrosine kinase-related diseases.
Isotope enrichment lenvatinib
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, (2020/03/09)
The invention discloses isotope enrichment lenvatinib, a pharmaceutically acceptable salt form thereof, and a treatment method using the isotope enrichment lenvatinib, and specifically relates to an isotope enrichment compound represented by a formula I o
A [...] synthetic method
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Paragraph 0043; 0051; 0053; 0060; 0062; 0069, (2019/05/22)
The invention provides a method of synthesizing [...]. First of all the invention to 4 - cyano - 3 - hydroxy aniline as the starting material, by dimethyl carbonate methylation, after third acid in the oximation reaction at room temperature, the conditions in the PPA shut-ring forms the 6 - cyano - 7 - methoxy - 4 - quinolinone, in thionyl chloride formed under the action of the 6 - cyano - 7 - methoxy - 4 - [...], under acidic conditions [...] cyano hydrolysis synthesis of one of the intermediates 6 - formamido - 7 - methoxy - 4 - chloroquinolin. Then the 4 - hydroxy - 2 chloroaniline with cyanogen bromide at low temperature 4 - hydroxy - 2 - chloro cyaniding amine, the 4 - hydroxy - 2 - chloro cyaniding amine with bearing-displacement generating Reeth reaction synthesis [...] another key intermediate 1 - (2 - chloro - 4 - hydroxy-phenyl) - 3 - ring propyl urea. Finally the two intermediate 6 - formamido - 7 - methoxy - 4 - chloroquinolin and 1 - (2 - chloro - 4 - hydroxy-phenyl) - 3 - ring propyl urea in the alkaline environment for carrying out the alkylation reaction [...]. This scheme has mild reaction conditions, no highly toxic reagent, environmental protection and the like.