- Synthesis of the Kinase Inhibitors Nintedanib, Hesperadin, and Their Analogues Using the Eschenmoser Coupling Reaction
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A novel synthetic approach involving an Eschenmoser coupling reaction of substituted 3-bromooxindoles (H, 6-Cl, 6-COOMe, 5-NO2) with two substituted thiobenzanilides in dimethylformamide or acetonitrile was used for the synthesis of eight kinase inhibitor
- Marek, Luká?,Váňa, Ji?í,Svoboda, Jan,Hanusek, Ji?í
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p. 10621 - 10629
(2021/07/31)
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- DRY POWDER FORMULATION FOR INHALATION COMPRISING FINE PARTICLE OF NINTEDANIB OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF
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The present invention relates to a dry powder formulation for inhalation comprising fine particles of nintedanib or a pharmaceutically acceptable salt thereof. Specifically, fine particles of nintedanib or a pharmaceutically acceptable salt thereof according to the present invention have an inhalable size and particle shape, are thermodynamically stable, and exhibit high emitted dose (ED) and fine particle fraction (FPF) values, thereby being able to be easily used as the dry powder formulation for inhalation.
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Paragraph 0065-0081
(2021/02/02)
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- METHODS FOR PREPARING NINTEDANIB AND INTERMEDIATES THEREOF
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The present application provides a method for preparing nintedanib. The method of the present application is carried out by using 4-halo-3-nitro-benzoic acid methyl ester (compound II) and 3-oxo-3-phenylpropionate (compound III) as raw materials, and prep
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- Preparation method of amino intermediate (by machine translation)
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Compared with an existing preparation method, the method for preparing. the amine-based (I) intermediate disclosed by the invention comprises the following, steps: carrying (III) out condensation, reduction and the like of the compound of. the formula I to obtain, the target compound (I), and 1 remarkably reducing the, content of the impurities in the obtained compound according to the, invention as compared with the existing preparation. method. (by machine translation)
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- Preparation method of nintedanib key intermediate
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The invention belongs to the technical field of pharmaceutical chemicals, and particularly relates to a preparation method of a nintedanib key intermediate compound II. A compound IV is reduced by adopting a common reaction reagent under the conditions of normal temperature and normal pressure, so that a high-purity compound II can be conveniently obtained. The adopted reaction conditions are mild, high-pressure equipment is avoided, the technical operation is simple, the conditions are mild, the process is safer and more environmentally friendly, and the feasibility of large-scale productionof nintedanib is greatly improved.
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Paragraph 0069-0074
(2020/10/27)
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- PROCESS FOR THE PREPARATION OF NINTEDANIB
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The present invention relates to a process for the preparation of nintedanib or salt thereof. The process comprising reacting compound of formula VI with acetic anhydride and triethyl ortho benzoate to obtain a compound of formula V; further reacting the compound of formula V with the compound of formula IV to obtain nintedanib the compound of formula I. The present invention also relates to a process to obtain crystalline compound of formula V.
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- Potential impurity compound of Nintedanib, as well as preparation method, application and detection method of potential impurity compound
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The invention relates to a potential impurity compound of Nintedanib, and a preparation method, application and detection method of the potential impurity compound. The structure of the potential impurity compound is shown in the formula (as shown in the specification). The invention aims to improve the quality standard of Nintedanib through study on impurities to guarantee the safe medication of Nintedanib. According to the preparation method disclosed by the invention, the pure potential impurity compound of Nintedanib is obtained, so that a reference substance for qualitative and quantitative analysis is provided for the detection of a finished Nintedanib product.
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- Preparation method of nintedanib ethyl sulfonate
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The invention discloses a preparation method of nintedanib ethyl sulfonate. The method comprises the steps of reacting by taking 2-oxoindole-6-carboxylic acid methyl ester, triethyl orthobenzoate and acetic anhydride as starting materials to obtain a compound; and carrying out condensation on (Z)-1-acetyl-3-(ethoxy (phenyl) methylene)-2-oxo indoline-6-carboxylic acid methyl ester and the starting material N-(4-aminophenyl)-N-methyl-2-(4-methyl piperazine-1-yl) acetamide to obtain nintedanib free alkali and carrying out salt-forming reaction of ethanesulfonic acid to prepare the nintedanib ethyl sulfonate. The method is short in step and easy to treat, and a high-quality nintedanib ethyl sulfonate crystal product is obtained without purification.
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Paragraph 0015; 0029
(2017/09/01)
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