302964-24-5Relevant articles and documents
SUBSTITUTED ARYLUREA COMPOUNDS FOR INDUCING APOPTOSIS AND COMPOSITION FOR ANTICANCER COMPRISING THE SAME
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, (2021/08/17)
The present invention relates to a substituted arylurea compound inducing apoptosis and an anticancer composition comprising the same. The present invention relates to a novel compound capable of preventing, treating and alleviating cancer diseases such as prostate cancer, breast cancer, lung cancer, colorectal cancer, and skin cancer by inhibiting apoptosis of cancer cells and inhibiting proliferation of cancer cells.
Protein kinase inhibitor and use thereof
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Paragraph 0091; 0098-0099; 0135; 0138-0139, (2021/01/21)
The present invention provides a compound of formula 1 having an activity of inhibiting protein kinase and its use.
Preparation process of dasatinib
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Paragraph 0055; 0056-0064; 0081; 0082; 0083; 0084-0086, (2019/06/27)
The invention relates to a preparation process of dasatinib. The preparation process includes the following steps that 3-ethyl propionate reacts with 2-chlorine-6-methylaniline under an alkaline condition to obtain a compound 3; the compound 3, copper bromide and thiourea react under action of hydroxyethyl-beta-cyclodextrin to obtain 2-amino-N-(2-chlorine-6-methyl phenyl) thiazole-5-formamide through a heating reaction; secondly, 4,6-dichloro-2-methyl pyrimidine reacts with N-hydroxyethyl piperazine, 2-amino-N-(2-chloro-6-methyl phenyl) thiazole-5-formamide sequentially in the presence of alkali, a catalytic system and an organic solvent, and a compound 1, namely dasatinib, is obtained. The conditions are mild, the steps are simple, the process is environmentally friendly, the yield is high, and the process is suitable for industrial production.
A reach [...] preparation method
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Paragraph 0033; 0051-0056; 0071-0076, (2019/07/01)
The invention relates to a preparation method of up to [...], the method comprises the following steps: 3 - ethyl oxo propionic acid under alkaline condition first with 2 - chloro - 6 - methylaniline reaction, then adding [...] copper solution reaction, to obtain compound 3; with the thiourea reaction, from 2 - amino - N - (2 - chloro - 6 - methyl phenyl) thiazole - 5 - carboxamide; after the 4, 6 - dichloro - 2 - methyl pyrimidine in alkali, catalytic system, organic solvents, successively with the N - hydroxyethyl piperazine, 2 - amino - N - (2 - chloro - 6 - methyl phenyl) thiazole - 5 - carboxamide reaction, to obtain compound 1, has reached the [...]. Mild condition of this invention, the step is simple, short reaction time, speed, friendly to the environment and have high yield, is suitable for industrial production.
Preparation method of dasatinib intermediate
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Paragraph 0041-0048; 0053; 0054, (2019/04/04)
The invention relates to a preparation method of a dasatinib intermediate. The method comprises the following steps: performing heating reflux on ethyl 3-oxopropanoate and 2-chloro-6-methylaniline under alkaline conditions, adding copper bromide, and performing warming reflux to obtain a compound 2; and cyclizing the compound 2 and thiourea in a solvent PEG 400 to obtain a target product, namely 2-amino-N-(2-chloro-6-methylphenyl)thiazole-5-carboxamide. The method involved in the invention has mild conditions, simple steps, environmental friendliness and high yield, and is suitable for industrial production.
Preparation process of dasatinib
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Paragraph 0034; 0053-0064; 0079; 0080, (2019/05/08)
The invention relates to a preparation process of dasatinib. The method comprises the following steps: enabling 3-oxopropionic acid ethyl ester to react firstly with 2-chlo-6-methylaniline under an alkaline condition, then adding a solvent dissolved with cupric bromide, and reacting to obtain a compound 3; cyclizing the compound 3 and thiourea in solvent water to obtain 2-amino-N-(2-chlo-6-methylphenyl)thiazole-5-formamide; and then synthesizing dasatinib from 4,6-dichloro-2-methyl pyrimidine, N-ethoxyl piperazine, and 2-amino-N-(2-chlo-6-methyl phenyl)thiazole-5-formamide through a one-pot method under the actions of an alkali K3PO4 and a catalyst 1-butyl-3-methylimidazole glycinate. The conditions are mild, the steps are simple, and the preparation process is environmentally-friendly, high in yield and suitable for industrial production.
Method for preparing dasatinib tablets
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Paragraph 0043-0056; 0069-0074, (2019/04/04)
The invention relates to a method for preparing dasatinib tablets. The method comprises the following steps: enabling 3-oxo-ethyl propionate to react with 2-chlorine-6-methylaniline under an alkali condition, further adding a solvent in which cupric bromide is dissolved to carry out a reaction, further adding thiourea, and cyclizing with a catalyst so as to obtain 2-amino-N-(2-chlorine-6-methyphenyl)thiazole-5-formamide; further synthesizing dasatinib tablets from 4,6-dichloro-2-methyl pyrimidine, N-ethoxy piperazine and 2-amino-N-(2-chlorine-6-methyphenyl)thiazole-5-formamide according to a one-pot method under the action of an alkali and an ionic liquid 1-butyl-3-methylimidazole glycinate. The method is mild in condition, simple in step, environmentally friendly, high in yield and applicable to industrial production.
Process for preparing dasatinib
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Paragraph 0041-0048; 0056-0063, (2019/03/08)
The invention relates to a process for preparing dasatinib. The process includes steps of carrying out heating reflux on 3-oxo-propionic acid ethyl ester and 2-chlorine-6-methylaniline under alkalineconditions, adding cupric bromide, carrying out temperature-rise reflux, adding thiourea and a catalyst heteropoly acid salt, and carrying out room-temperature stirring reaction to obtain 2-amine-N-(2-chlorine-6-methyl phenyl)thiazole-5-formamide; carrying out 'one-pot reaction' on the 2-amine-N-(2-chlorine-6-methyl phenyl)thiazole-5-formamide, 4, 6-dichloro-2-methylpyrimidine and N-hydroxyethyl piperazine under the effects of catalysts to obtain the dasatinib. The process has the advantages of mild condition, simple step, environmental friendliness, high yield and applicability to industrialproduction.
Scalable and impurity-free process for dasatinib: Src and BCR-Abl inhibitor
Buchappa,Sagar Vijay Kumar,Durga Prasad,Aparna
, p. 1621 - 1628 (2018/06/12)
An efficient, telescopic, impurity-free and scalable process for Bcr-Abl and Src family tyrosine kinase inhibitor for synthesis of Dasatinib with high yield and purity is described.
AN IMPROVED PROCESS FOR THE PREPARATION OF DASATINIB POLYMORPH
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Page/Page column 9-10, (2018/06/22)
The present invention is related to an improved process for the preparation of dasatinib anhydrous crystalline Neat form N-6 with high purity and high yield. The present invention also relates to purification of dasatinib crystalline Neat form N-6.