Phosphoramidates: Features of the formation mechanism and the relationship structure-bioaction
作者:V. I. Krutikov、A. V. Erkin、V. V. Krutikova
DOI:10.1134/s1070363212050039
日期:2012.5
Mechanism of the synthesis of phosphoramidates by Todd-Atherton reaction is based on the primary interaction of a polyhaloalkane with the highly basic amine to form a 1:1 associate. The subsequent attack by the associate on the hydrophosphoryl compound of "symmetric" structure leads to the formation of the target compounds in high yields. The test of the effect of dialkyl hexamethylene- and dialkyl(pyridin-2-yl)-phosphoramidates in vitro against the strains of a number of the producents of pathogenic bacteria and mycotoxins showed that the high level of biological activity of the target compounds is correlated well with the physicochemical parameters characterizing their structure.