I. Yu. Belavin

Some problems of the teaching of organic chemistry in universities of Russia

Original Russian Text

Trimethylchlorosilane catalyzed addition of azole derivatives to 1-vinyl-2-pyrrolidone and pharmacological activity of products formed

l-(2-Oxopyrrolidin-l-yl)-l-(3,5-dimethylpyrazol-l-yl)-ethane (I). A mixture of 9.6 g (0.i mole) of 3,5-dimethylpyrazole, ii.i g (0.i mole) of l-vinyl-2-pyrrolidone and 5 ml of Me3SiCI was heated for 3 h at the boiling point. After cooling 50 ml of ether was added. The crystals that separated out were filtered off and washed with ether. Yield, 19 g (95%) of product, mp I16.5-I17.5~ C~IHITN30. IR spectrum, ~max, cm-1:1678 (C=O), 1558 (the pyrazole system), PMR spectrum, 6, ppm: 1.72 d (CH3CH) , 6.26 q (CHCH3), J = 7 Hz.

Synthesis and anticonvulsant activity of 5-aminopyrazoles

Compounds which contain the pyrazole ring exhibit a variety of biological activities (anaigesic, antiinflammatory, etc.). The 5-aminopyrazoles are also potentially biologically active substances which are readily obtained by the cyclization of dimers of nitriles derived from aliphatic carboxylic acids with substituted hydrazines [i]. A study of the literature on these compounds indicates that until the present work, there was no convenient method for the preparation of dimeric nitriles.