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Benzamide compounds containing acetenyl group
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A compound and alkyl technology, applied in the field of medicine, can solve problems such as drug resistance
Inactive Publication Date: 2017-05-24
ZHEJIANG DADE PHARMACEUTICAL GROUP CO LTD
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[0006] In view of the large number of protein kinase inhibitors and the variety of proliferative and other protein kinase-related diseases, and the emergence of resistance to existing drugs, we need to develop new classes of compounds to be used as protein kinase inhibitors, For the treatment of these protein kinase-associated diseases
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[0067] In a three-necked flask, add 500g of 2-trifluoromethylbenzaldehyde, 1500ml of absolute ethanol, 50g of tetrabutylammonium bromide, stir to dissolve, and keep the temperature at 0°C, add 150g of sodiumborohydride in batches, each time 30g. Stir for 30 minutes after the addition, then raise the temperature to 40° C., react for 2 hours, follow TLC, and the reaction is complete. Concentrate under reduced pressure, add 500ml of water, stir for 30min, add 1500ml of ether for extraction, wash with water, dry over anhydrousmagnesiumsulfate, filter, and concentrate to obtain 450g of 2-trifluoromethylbenzyl alcohol with a yield of 89%. MS (M+1) = 177.04. 1 HNMR data (300MHz, CDCl 3 ): 7.50-7.33 (m, 4H, benzene ring), 5.87 (s, 1H, -OH), 4.20 (s, 2H, -CH 2 -).
[0068] ii) 4-nitr...
Embodiment 2
[0085] 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((4-(piperidin-3 Preparation of -yl)pyrimidin-2-yl)ethynyl)benzamide methanesulfonate
[0086] Dissolve 5.4 g of the compound obtained in Example 1 in 250 ml of acetone, add 3 g of citric acid monohydrate, stir to dissolve, heat to reflux for 1 h, solid precipitates, cool, and filter. Dissolve the filtered solid in 500ml of water, add dropwise 1% sodiumhydroxide solution, adjust the pH value to about 9, filter, and repeat the above operation once for the obtained solid.
[0087] Redissolve the purified product in acetone, add an appropriate amount of methanesulfonic acid, stir, and heat to reflux for 1 hour. Solids are precipitated, cooled, filtered, and dried to obtain the product.
[0090] Purified 4-methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((4-( Dissolve piperidin-3-yl)pyrimidin-2-yl)ethynyl)benzamide in ethanol, add 10% hydrochloric acid solution, stir, heat to 60°C, react for 2h, after the reaction, remove ethanol by distillation under reduced pressure , add acetone, stir for 30min, a solid precipitates out, filter and dry to obtain the product.
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Abstract
The invention provides acetenyl group-containing benzamide compounds as shown in a formula (I) and used for treating or preventing diseases related to proteinkinase, and medicinal salts or configurational isomers thereof. A connection group L<1>, a ring A and substituents R<1>, R<2>, R<3>, R<4> and R <5> in the formula (I) are as defined in the specification. The invention also discloses a preparation method and a pharmaceutical composition of the compounds as shown in the formula (I), and application of the compounds to preparation or prevention of drugs used for preventing diseases related to proteinkinase.
Description
technical field [0001] The present invention relates to the field of medical technology, in particular to a class of benzamide compounds containing ethynyl groups, or pharmaceutically acceptable salts of such compounds, used alone or in combination with one or more other pharmaceutically active compounds Treatment of diseases, especially leukemia, responsive to inhibition of proteinkinase activity. Background technique [0002] Protein kinases are a class of phosphotransferases whose role is to transfer the γ-phosphate group of ATP to specific amino acid residues of the substrate to phosphorylate proteins. These phosphorylation functions as molecular on / off switches that can modulate or modulate the biological function of the target protein, ultimately being triggered in response to a variety of extracellular and other stimuli. These stimuli include environmental and chemical stress signals (e.g. shock, heat shock, UV exposure, bacterial endotoxin and H 2 o 2 ), cytokine...
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