One-step synthesis of 4-methyl-2-substituted quinazoline-3-oxides via polyphosphoric acid catalyzed acylation of electron-rich anilides with nitroethane
作者:Igor Yu Grishin、Alexander V. Aksenov、Nicolai A. Aksenov、Yuriy I. Grishin、Alexander V. Leontiev、Dmitrii A. Aksenov
DOI:10.1016/j.tet.2023.133784
日期:2024.1
A diverse set of 4-methyl-2-substituted quinazoline-3-oxides has been prepared usingpolyphosphoricacid both as a reaction medium and a Brønsted-acid catalyst. The reaction proceeds in a domino fashion via the formation of a corresponding oxime followed by exo-trig cyclization and elimination of a water molecule which leads, ultimately, to the target N-oxide heterocycles.
LACTATE DEHYDROGENASE INHIBITOR AND ANTIEPILEPTIC DRUG CONTAINING SAME
申请人:National University Corporation Okayama University
公开号:EP3257510A1
公开(公告)日:2017-12-20
The invention provides a lactate dehydrogenase inhibitor that makes it possible to suppress refractory epilepsy in which conventional antiepileptic drugs are ineffective, and an antiepileptic drug containing said inhibitor. The lactate dehydrogenase inhibitor of the invention contains a compound represented by formula (III); i.e., isosafrole or a compound having isosafrole as a scaffold, and the antiepileptic drug of the invention has these compounds as an active ingredient.
Effects of the structure of primary nitroalkanes and reaction conditions on the selectivity of acylamination of arenes in polyphosphoric acid
作者:A. V. Aksenov、I. Yu. Grishin、D. A. Aksenov、Yu. I. Grishin、I. V. Aksenova、N. A. Aksenov
DOI:10.1007/s11172-024-4277-8
日期:2024.6
The mechanism of acylamination of arenes with nitroalkanes in polyphosphoricacid has been clarified. The influence of the concentration of polyphosphoricacid, the structure of the starting compounds, and temperature on the result of the Beckmann rearrangement, which makes it possible to shift the reaction towards either benzamides or anilides, has been assessed.