SYNTHESIS AND ANALGESIC ACTIVITY OF BIS(3,4-DIHYDROQUINOXALIN-2(1<i>H</i>)-ONE) AND BIS(3,4-DIHYDRO-2<i>H</i>-1,4-BENZOXAZIN-2-ONE) DERIVATIVES

Authors

  • Иван Вячеславович Кулаков ФГБОУ ВПО "ОмГУ им. Ф.М.Достоевского"

DOI:

https://doi.org/10.1007/4088

Keywords:

3, 5-diacetyl-2, 6-dimethylpyridine, 4-dihydro-2H-1, 4-benzoxazin-2-one, 4-dihydroquinoxalin-2(1H)-one, analgesic activity, X-ray structural analysis.

Abstract

An ester condensation between 3,5-diacetyl-2,6-dimethylpyridine and an excess of diethyl oxalate was used for the preparation of 4,4'-(2,6-dimethylpyridine-3,5-diyl)bis(2-hydroxy-4-oxobut-2-enoate). The synthesized hydroxyester was shown to readily react with оphenylenediamine and о-aminophenol with the formation of bis(3,4-dihydroquinoxalin-2(1H)-one) and bis(3,4-dihydro-2H-1,4-benzoxazin-2-one) derivatives, which showed superior in vivo analgesic activity compared to the reference drug, metamizole sodium.

 

Author Biography

Иван Вячеславович Кулаков, ФГБОУ ВПО "ОмГУ им. Ф.М.Достоевского"

д.х.н., профессор кафедры органической химии

Published

2017-11-27

Issue

Section

Original Papers