PROCESS FOR PREPARING AMINOGLYCOSIDE DERIVATIVES, NOVEL DERIVATIVES OBTAINED AND PHARMACEUTICAL COMPOSITIONS CONTAINING SUCH DERIVATIVES

摘要

This invention relates to a process for preparing 2 min -hydroxy-2 min - desamino-4,6-di-O-(aminoglycosyl) -1,3-diaminocyclitols having a 6 min -amino function and pharmaceutically acceptable acid addition salts thereof, to novel compounds and salts obtained by this process; and to novel antibacterially active compositions comprising such novel compounds or salts. The process comprises reacting the corresponding N-protected (except the 2 min -amino)-4,6-di-O- (aminoglycosyl)-1,3,-diaminocyclitol with hydrogen peroxide in the presence of tungstate ion, followed by cleavage of the thereby formed 2 min -oximino derivative and by reduction of the resulting 2 min -oxo derivative and by removal of the N-protecting groups. The preferred group of novel compounds obtained by this process are the 1-N- ( omega -amino- alpha - hydroxyalkanoyl) -2 min -hydroxy-2 min - desamino-4,6-di-O- (aminoglycosyl)- 1,3-diaminocyclitols. The compounds obtained by the process of this invention exhibit antibacterial activity