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Preparation method and use of dihydropteridine-containing diketone skeleton derivative
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A technology of dihydropteridine and derivatives, which is applied in the application of medicines, the preparation of medicines for the treatment and/or prevention of cancer, can solve the problems of high homology and the mode of administration of PLK1 small molecule inhibitors, etc.
Active Publication Date: 2021-06-01
SHENYANG PHARMA UNIVERSITY
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However, due to the high homology between PLK subtypes and the problems caused by the way of administration, no small molecule inhibitors of PLK1 have been approved for marketing so far. There is an urgent need to find more new and efficient PLK1 inhibitors to provide new treatments for tumors and other diseases. the choice of
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[0100] 50g (259mmol) 2,4-dichloro-5-nitropyrimidine, 43.5g (518mmol) NaHCO3, 200mL DCM were added to the three-necked flask, and the DCM solution of 26.4g (311mmol) cyclopentylamine was added dropwise to the above-mentioned In the reaction solution, react at room temperature for 10 h. After the reaction was completed, the reaction solution was poured into 200 mL of water, the organic layer was separated, the aqueous layer was extracted twice with 100 mL of DCM, the organic layers were combined, dried over anhydroussodiumsulfate, the solvent was evaporated to dryness, diethyl ether was added to the residue, and a light yellow solid was precipitated , filtered by suction, and dried to obtain 53.27g of a light yellow solid, yield 85.0%, m.p.: 125.2–126.6°C, MS (ESI) m / z: 243.3 [M+H] + .
[0101] Step B: Synthesis of 2-chloro-4-cyclopentylamino-5-aminopyrimidine (3)
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Abstract
The present invention relates to dihydropteridinedione derivatives represented by general formula I and their optical isomers, pharmaceutically acceptable salts, solvates or prodrugs, their preparation methods and compounds represented by general formula I as active A pharmaceutical composition of ingredients, wherein the substituent R 1 , R 2 , R 3 , Ar have the meaning given in the description. The present invention also relates to compounds of the general formula I having a strong PLK1 inhibitory effect, and also relates to the preparation of such compounds and their optical isomers and pharmaceutically acceptable salts for the treatment and / or prevention of PLK1 abnormal expression. Application in medicines for diseases, especially in the preparation of medicines for treating and / or preventing cancer.
Description
technical field [0001] The present invention relates to dihydropteridinedione derivatives and their optical isomers, pharmaceutically acceptable salts, solvates or prodrugs, their preparation methods and pharmaceutical compositions containing the compounds. The present invention also relates to the strong PLK1 kinaseinhibitory effect of the compound, and also relates to the preparation of such compounds and their optical isomers and pharmaceutically acceptable salts for the treatment and / or prevention of diseases caused by abnormal expression of PLK1 The application in the medicine of medicine, especially the purposes in the preparation of the medicine of treating and / or preventing cancer. Background technique [0002] Cancer, also known as malignant tumor, is a malignant disease caused by abnormal differentiation and proliferation of normal tissue cells. Cancer is the second leading cause of death worldwide and is becoming a growing public health problem. Therefore, rese...
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