362656-11-9Relevant articles and documents
HETEROCYCLIC COMPOUNDS AS KINASE INHIBITORS
-
Paragraph 0600; 0603, (2021/01/23)
Heterocyclic compounds as CDK4 or CDK6 or other CDK inhibitors are provided. The compounds may find use as therapeutic agents for the treatment of diseases and may find particular use in oncology.
Preparation method for 1-(4-cyclopentylamine-2-methylmercapto-pyrimidine-5-)ethyl ketone
-
Paragraph 0057; 0058; 0059; 0065; 0066, (2017/08/28)
The invention discloses a preparation method for 1-(4-cyclopentylamine-2-methylmercapto-pyrimidine-5-)ethyl ketone. The method comprises the following steps of: (a) adding 4-cyclopentylamine-2-methylmercapto-pyrimidine-5-ethyl formate disclosed by a formula (1) and alkali into organic solvent to react to obtain 4-cyclopentylamine-2-methylmercapto-pyrimidine-5-methanoic acid disclosed in a formula (2); (b) carrying out condensation reaction on the 4-cyclopentylamine-2-methylmercapto-pyrimidine-5-methanoic acid disclosed in the formula (2) and N,O-dimethylhydroxylamine hydrochloride disclosed in a formula (3) to obtain a 4-cyclopentylamine-N-methoxyl-N-methyl-2-methylmercapto-pyrimidine-5-formamide disclosed in a formula (4); and (c) enabling the 4-cyclopentylamine-N-methoxyl-N-methyl-2-methylmercapto-pyrimidine-5-formamide disclosed in the formula (4) to react with methyl magnesium bromide to obtain the1-(4-cyclopentylamine-2-methylmercapto-pyrimidine-5-)ethyl ketone disclosed in a formula (5). The preparation method disclosed by the invention has the advantages of being low in cost and convenient and safe in operation and is easy in large-scale industrial production, and column chromatography isolation purification is not required during postprocessing.
Novel important intermediate for anticancer drug palbociclib and compounding process
-
Paragraph 0036-0038, (2017/08/29)
The invention discloses a compounding process for a novel important intermediate for anticancer drug palbociclib. The compounding process includes allowing a compound 1 and a compound 2 to react with each other at a time with high yield under the action of Grignard reagents to obtain a compound 3, and allowing the compound 3 to react with R7CH2COOR3 to obtain a compound 4. The compounding process has a short path, and only two reaction steps, from the initial raw material 1 to the key intermediate pyridino-pyrimidine-7-ketone derivative 4, are needed; raw materials are cheap, reaction process is harmless to the environment, overall yield is high, and the compounding process is suitable for mass production.