ES428892A1 - Procedure for the preparation of new pseudotrisacaridos. (Machine-translation by Google Translate, not legally binding) - Google Patents

Abstract

Procedure for the preparation of new pseudotrisaccharides, particularly 1-N substituted derivatives of 4,6-di- (aminoglycosyl) -1,3-diaminocyclitols gentamicin A, gentamicin B, gentamicin B1, gentamicin C1, gentamicin C1a, gentamicin C2, Gentamicin C2a, Gentamicin C2b, Gentamicin X2, Sisomycin, Verdamicin, Tobramycin, G-418 Antibiotic, 66-40B Antibiotic, JI-20A Antibiotic, JI-20B Antibiotic, G-52 Antibiotic, Mutamycin 1,, mutamicin 4, mutamicin 5 and mutamicin 6, in which the substituent is **(See formula)** where X is hydrogen, alcoholic, alkenyl, cycloalkyl, cycloalkoxylalkyl, hydroxyalkyl, aminoalcohyl, N-alcoholylaminoalcohyl, aminohydroxyalkyl, N-alcoholylaminohydroxyalkyl, phenyl, benzyl or tolyl, with said aliphatic radicals being up to seven carbon atoms and, if, and, if, they are aliphatic radicals with and if hydroxy, bearing the substituents on different carbon atoms, and of the pharmaceutically acceptable acid addition salts thereof, which method comprises treating one of the 4, 6-di- (aminoglycosyl) -1,3-diamino-cyclitols mentioned above which may have amino protecting groups at any position other than position 1, with an aldehyde of the formula **(See formula)** where X is a group as defined above for X in which any amino or hydroxy group present may be protected, in the presence of a hydride donor reducing agent and, if required, remove all protecting groups present in the molecule, being followed by the last step of the process by isolation of the derivative as is or in the form of a pharmaceutically acceptable acid addition salt. (Machine-translation by Google Translate, not legally binding)