23-O-SUBSTITUTED MYCAMINOSYLTYLONOLIDE DERIVATIVE AND PREPARATION THEREOF

摘要

NEW MATERIAL:A compound expressed by formulaII(R is quinolyl, benzotriazolyl, alpha-lower alkylbenzylideneimino or pteridino). EXAMPLE:23-O-(8-Quinolyl)mycaminosyltylonolide. USE:An antimicrobial agent against Gram-positive and Gram-negative bacteria capable of exhibiting powerful activity particularly against Gram-positive bacteria. PREPARATION:A mycaminosyltylonolide derivative, expressed by formula II (A is protected aldehyde), and having protected aldehyde is reacted with a compound expressed by formula III, preferably in the presence of a condensing agent, e.g. triphenylphosphine, in a solvent, e.g. tetrahydrofuran (THF), usually at room temperature to give a compound expressed by formula IV. The protecting group of the aldehyde is then removed.