- UREA-SUBSTITUTED AROMATIC RING-LINKED DIOXANE-QUINAZOLINE AND -LINKED DIOXANE-QUINOLINE COMPOUNDS, PREPARATION METHOD THEREFOR AND USE THEREOF
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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.
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Paragraph 0090-0091
(2020/01/22)
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- Method for refining Lenvatinib mesylate
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The invention discloses a method for refining Lenvatinib mesylate. The method for refining the Lenvatinib mesylate, provided by the invention, comprises the following step: subjecting a solution formed by an organic solvent and crude Lenvatinib mesylate t
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- Isotope enrichment lenvatinib
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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
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- PROCESS FOR THE PREPARATION OF LENVATINIB
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The present invention relates to a process for the preparation of Lenvatinib of formula (I) from 4-amino-3-chloro-phenol and 4-chloro-7-methoxyquinoline-6-carboxamide.
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Page/Page column 5-6
(2020/04/09)
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- Substituted urea compound and pharmaceutically acceptable salts or solvates thereof, application for substituted urea compound and pharmaceutically acceptable salts or solvates of substituted urea compound, and pharmaceuticals and pharmaceutical compositi
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The invention provides a substituted urea compound, and pharmaceutically acceptable salts or solvates thereof. The invention also provides an application of the substituted urea compound, the pharmaceutically acceptable salts or the solvates of the substi
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- A [...] synthetic method
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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.
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- Method for synthesizing lenvatinib
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The invention belongs to the field of chemical pharmacy, and specifically relates to a method for synthesizing lenvatinib. The method comprises the following steps: step 1, taking 4-aminosalicylic acid as a raw material, and preparing 4-chloro-7-methoxyquinoline-6-formamide through methylation, condensation with meldrum's acid, high-temperature cyclization, chlorination and ammoniation; step 2, taking 3-chloro-4-aminophenol as a raw material, and reacting with phenyl chloroformate and cyclopropylamine to obtain 1-(2-chloro-4-hydroxy phenyl)-3-cyclopropyl urea; and step 3, enabling the 4-chloro-7-methoxyquinoline-6-formamide prepared in step 1 to react with the 1-(2-chloro-4-hydroxy phenyl)-3-cyclopropyl urea prepared in step 2 under action of potassium tert-butoxide to obtain the lenvatinib. The invention provides a brand-new route for synthesising the lenvatinib. The used reagent is cheap and is easily available, is simple in operation, has a yield higher than that of other methods, and is easy for industrial production.
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Paragraph 0030; 0031
(2019/03/28)
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- Deuterated compound, salt, preparation method, drug composition and application thereof
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The invention discloses a compound with the structure shown in the formula (I) and pharmacologically acceptable salt. The invention further provides a preparation method of the compound shown in the formula (I) and a drug composition containing the compou
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- [...] intermediate and its preparation and [...] preparation (by machine translation)
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The present invention relates to the field of drug synthesis, discloses a [...] key intermediate 1 - (2 - chloro - 4 - hydroxy-phenyl) - 3 - ring propyl urea and its preparation and [...] preparation. The music-cutting of the Buddhist intermediate, its pu
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Paragraph 0074; 0078-0080; 0088; 0092-0094; 0102; 0106-0108
(2019/01/08)
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- Preparation method of lenvatinib
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The invention belongs to the field of medical chemistry, and provides a preparation method of a compound of lenvatinib. The method is characterized by comprising the following steps that (1) under the existence of an organic solvent and an alkali reagent,
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- Polymorph of 4-[3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy]-7-methoxy-6- quinolinecarboxamide and a process for the preparation of the same
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A polymorph (A) of 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide, having a diffraction peak at a diffraction angle (2θ±0.2°) of 15.75° in a powder X-ray diffraction; and a polymorph (B) of 4-[3-chloro-4-(cyclopropy
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Page/Page column 5
(2008/06/13)
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- Amorphous salt of 4-(3-chiloro-4-(cycloproplylaminocarbonyl)aminophenoxy)-7-method-6-quinolinecarboxamide and process for preparing the same
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An amorphous form of a salt of 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide.
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Page/Page column 5
(2008/06/13)
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- MEDICINAL COMPOSITION
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A pharmaceutical composition comprising: an active ingredient consisting of 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide, salt thereof, or solvate of the foregoing; and (i) a compound, a 5% (w/w) aqueous solution
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Page/Page column 12
(2008/06/13)
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- UREA DERIVATIVE AND PROCESS FOR PRODUCING THE SAME
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A process for preparing a compound (C) represented by the following formula: wherein R1 represents hydrogen, C1-6 alkyl or C3-8 cycloalkyl, and R2 represents hydrogen or methoxy,characterized by reacting a compo
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Page/Page column 7-8
(2008/06/13)
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- CRYSTAL OF SALT OF 4-(3-CHLORO-4-(CYCLOPROPYLAMINOCARBONYL)AMINO-PHENOXY)-7-METHOXY-6-QUINOLINECARBOXAMIDE OR OF SOLVATE THEREOF AND PROCESSES FOR PRODUCING THESE
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A crystal of a 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide hydrochloride, hydrobromide, p-toluenesulfonate, sulfate, methanesulfonate or ethanesulfonate, or a solvate thereof.
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Page/Page column 15
(2008/06/13)
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- AMORPHOUS SALT OF 4-(3-CHLORO-4-(CYCLOPROPYLAMINOCARBONYL)-AMINOPHENOXY)-7-METHOXY-6-QUINOLINECARBOXAMIDE AND PROCESS FOR PRODUCING THE SAME
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An amorphous salt of 4-(3-chloro-4-(cyclopropylaminocarbonyl)-aminophenoxy)-7-methoxy-6-quinolinecarboxamide.
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Page/Page column 11
(2008/06/13)
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