ES443468A1 - PROCEDURE FOR THE PREPARATION OF ACTIVE PSEUDOTRISACCHARIDES AS ANTIBIOTICS. - Google Patents

Abstract

Procedure for the preparation of pseudotrisaccharides active as antibiotics that have the general formula **(See formula)** and its pharmaceutically acceptable acid addition salts and its Schiff-based oxazolidine derivatives, wherein, in the formula, R 2 represents hydrogen or hydroxy; R3 represents hydroxy, amino or lower alcohol-monosubstituted amino; R4 represents hydrogen or lower alcohol; and R5 represents hydroxy, amino or lower alcohol-monosubstituted amino with the conditions that (a) when R2 is hydroxy, it is hydrogen or methyl and R3 is amino, then R5 must be lower alcohol-monosubstituted amino and (b) when both R2 Since R3 are hydroxy and R4 is hydrogen or methyl, then R5 must be hydroxy or lower alcohol-monosubstituted amino; comprising subjecting a compound of the general formula II **(See formula)** where R4 is as defined above, R7 represents hydrogen or -OR11, each of R8 and R9 represents -OR11, or -NRR10, where R is hydrogen or alcoholic or less, R10 represents hydrogen or an amino protecting group and R 11 represents hydrogen or a hydroxy protecting group and in which R10 in position 3 "together with R11 in position 4" or both R10 in positions 1 and 3 together can represent a protecting group and in which at least one protecting group is present in the molecule, with the provisos that (a) when R7 is -OR11, R4 is hydrogen or methyl and R8 is -NHR10, then R9 must be -NRR10 representing R lower alcohol, and (b) when both R7 and R8 are -OR11, and R4 is hydrogen or methyl, then R9 must be -OR11, or 2 11-NRR10, R representing lower alcohol, to a removal of all protecting groups present in the molecule, followed, if desired, by preparation of a salt by addition of pharmaceutically acceptable acid or an oxazolidine derivative of base Schiff's analysis of the compound of formula I thus obtained. (Machine-translation by Google Translate, not legally binding)