- Preparation process of dasatinib
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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.
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Paragraph 0043; 0044; 0045-0054; 0075; 0076-0080
(2019/06/27)
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- Theramutein modulators
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This invention relates to agents that are inhibitors or activators of variant forms of endogenous proteins and novel methods of identifying such variants. Of particular interest are inhibitors and activators of endogenous protein variants, encoded by genes which have mutated, which variants often arise or are at least first identified as having arisen following exposure to a chemical agent which is known to be an inhibitor or activator of the corresponding unmutated endogenous protein.
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Page/Page column 172
(2010/02/17)
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- THERAMUTEIN MODULATORS
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This invention relates to agents that are inhibitors or activators of variant forms of endogenous proteins and novel methods of identifying such variants. Of particular interest are inhibitors and activators of endogenous protein variants, encoded by genes which have mutated, which variants often arise or are at least first identified as having arisen following exposure to a chemical agent which is known to be an inhibitor or activator of the corresponding unmutated endogenous protein.
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Page/Page column 204
(2008/12/07)
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