| 摘要 |
Disclosed are 5-oxo-N-aryl-2,3-disubstituted-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidin-7-carboxamides of general formula,wherein R= H; CH; 4-Cl-CH; 4-F-CH; 4-CHO-CH; 4-CH-CH; 4-Br-CH; 3-Cl-CH;R= CH; CH; 4-Cl-CH; 4-F-CH; 4-CHO-CH; 4-CH-CH; 4-Br-CH; 3-Cl-CH; 2-Cl-CH; 2-CHO-CH; 3,4-di-CHO-CH;Ar = CH; 4-Cl-CH; 2-Cl-CH; 4-CHO-CH; 3-CHO-CH; 2,4-di-CHO-CH; 3,4-OCHO-CH; 3-F-CH; 3-Cl-CH; 2-F-CH; 4-Br-CH; 4-EtOC-CH; 2,4-di-CH-CH; 2,5-di-CH-CH; 3,4-di-CH-CH; 3,4-di-F-CH; 2,4-di-F-CH; 2,4-di-Cl-CH; 4-F-CH; 4-CF-CH; 3-CF-CH; 2-CHO-CH; 2-CF-CH; 2-CHO-5-Cl-CH; 4-CHO-3-Cl-CH; 2,5-CHO-CH; 3,4-di-CHO-CH,and a process for the preparation thereof that involves condensation of equimolar quantities of 3,4-disubstituted-5-aminopyrazoles with N-arylmaleimides in N,N-dimethylformamide at boiling for 5-10 minutes. The separation of desired product is carried out by precipitation with acetone. The invention enables to reduce process time, increase quality of compounds and reaction yields thereof and provides wide range of pyrazolopyrimidines for medicine, pharmacology and biology. |
