89943-02-2Relevant articles and documents
(PYRIDIN-2-YL)AMINE DERIVATIVES AS TGF-BETA R1 (ALK5) INHIBITORS FOR THE TREATMENT OF CANCER
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, (2020/07/15)
The present invention relates to pharmaceutical compounds, compositions and methods, especially as they are related to compositions and methods for the treatment and/or prevention of a proliferation disorder associated with ΤGFβR1 activity, such as a cancer or fibrosis. The invention provides compounds of Formula (I) and Formula (II) as further described herein having an acidic moiety that enhances tissue specificity for targeted tissues and organs. The invention includes pharmaceutical compositions, pharmaceutical combinations, and methods of use of these compounds for treating conditions including cancer or fibrosis.
A 2, 5 - dimethyl -3 - bromo pyridine synthesis method
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, (2019/05/28)
The invention relates to the field of organic chemistry, in particular to a 2, 5 - dimethyl - 3 - bromo pyridine synthesis method, comprises the following steps: 1, malonic acid diethyl ester and alkali metal reaction to produce salt, then dropwise 2 methyl - 3 - nitro - 5 chloro pyridine to a toluene solution of a condensation reaction, after decarboxylation under acidic conditions shall be 2, 5 - dimethyl - 3 - nitro pyridine; 2, 2, 5 - dimethyl - 3 - nitro pyridine in under the catalysis of the Pd/C, methanol as the solvent, hydrogen reduction, filtered, the filtrate is concentrated, shall be 2, 5 - dimethyl - 3 - aminopyridine; 3, 2, 5 - dimethyl - 3 - aminopyridine first with an acid generating salt, cooling to - 9 °C - 4 °C, [...], drops the instillment sodium nitrite aqueous solution, pH adjusting solution is dropped is alkaline, and then extracted, drying, concentration, shall be 2, 5 - dimethyl - 3 - bromo pyridine. The method of the invention is beneficial effect: mild reaction conditions, high yield, and raw materials are easy, and the cost is low, the process route is short, and has industrial prospects.
A 2, 5 - dimethyl - 3 - bromo pyridine synthesis method (by machine translation)
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, (2017/09/26)
The invention relates to the field of organic chemistry, in particular to a 2, 5 - dimethyl - 3 - bromo pyridine synthesis method, comprises the following steps: 1, malonic acid diethyl ester and alkali metal reaction to produce salt, then dropwise 2 methyl - 3 - nitro - 5 chloro pyridine to a toluene solution of a condensation reaction, after decarboxylation under acidic conditions shall be 2, 5 - dimethyl - 3 - nitro pyridine; 2, 2, 5 - dimethyl - 3 - nitro pyridine in under the catalysis of the Pd/C, methanol as the solvent, hydrogen reduction, filtered, the filtrate is concentrated, shall be 2, 5 - dimethyl - 3 - aminopyridine; 3, 2, 5 - dimethyl - 3 - aminopyridine first with an acid generating salt, cooling to - 9 °C - 4 °C, instillment fluid bromine, drops the instillment sodium nitrite aqueous solution, pH adjusting solution is dropped is alkaline, and then extracted, drying, concentration, shall be 2, 5 - dimethyl - 3 - bromo pyridine. The method of the invention is beneficial effect: mild reaction conditions, high yield, and raw materials are easy, and the cost is low, the process route is short, and has industrial prospects. (by machine translation)