| 摘要 |
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to an improved method for preparing 2-arylamino-4-hetarylpyrimidines of formula (I) which possess inhibitory action on serine-threonine kinase Haspin on the enzymatic level, and may be used as drug substances for oncological diseases. In formula(I), wherein Het =,,,,,,,,,,,R=H; 2-Me; 3-Me; 4-Me; 2,3-di-Me; 2-MeO; 3-MeO; 4-MeO; 4-EtO; 4-PhO; 2-Cl; 3-Cl; 4-Cl; 4-F; 2-Me, 3-Cl. The method consists in a reaction of related hetarylmethylketone and N,N-dimethylformamide dimethylacetale on boiling of reagents in isopropyl alchohol for 6 hours to produce 3-dimethylamino-1-hetaryl-2-propen-1-ones with adding in situ related aryl guanidine and further boiling for 2 hours. The process is conducted at molar ratio (mole) of hetarylmethylketone: N,N-dimethylformamide dimethylacetale : aryl guanidine = 1:1.5:1.EFFECT: method simplifies the process due to cutting a process time and reducing consumption of the initial ingredients.6 ex |
