| 摘要 |
The invention relates to organic chemistry, in particular to the general process for preparation of the previously unknown 4-aryl 1,4,5,10- tetrahydro pyrazole [3,4-b][1,5] benzodiazepines, which can be used in medicine, and also as a starting substances for the synthesis of different types of pyrazole- and 1,5-benzodiazepine-containing compounds.The basis of the invention is simple and convinient from synthesis point of view process for preparation of 4-aryl 1,4,5,10-tetrahydro pyrazole [3,4-b][1,5] benzodiazepines of the general formula 1, (1)where R–cyanoethyl group or phenylic radical, andАr–aromatic or heteroaromatic radical.The process is rimplemented according to the single-stage reaction scheme. It is based on the reaction of cyclocondensation of 5-(amino aniline) pyrazoles with aromatic aldehydes. The process is occured at the boiling of reagents in ethanol or toluene in the presence of catalytic amount of acetic acid and is completed in 1,5 hour. Product yields are 72-97 %. |
