Selective acylation of the c-1 amino group of aminoglycoside...

Details Selective acylation of the c-1 amino group of aminoglycoside... Selective acylation of the c-1 amino group of aminoglycoside...

C - Chemistry, Metallurgy

07

H

260/230.56

C07H 15/22 (2006.01) C07H 15/236 (2006.01)

Patent

CA 1045129

ABSTRACT OF THE DISCLOSURE The disclosure describes a process for the preparation of 1-N-substituted derivatives of 4,6-di-(aminoglycosyl)-1,3- diaminocyclitols, wherein the 1-N-substituent is an acyl group having 1 to 8 carbon atoms, which may be monosubstituted by amino or hydroxy or disubstituted by amino and hydroxy at different carbon atoms, and of the pharmaceutically acceptable acid addition salts thereof. The process comprises treating a 4,6-di-(aminoglycosyl)-1,3-diaminocyclitol, which is partially neutralized by formation of an acid addition salt, with an acylating agent containing the above defined acyl group, and then isolating the 1-N-derivative as such or as a pharmaceutical- ly acceptable acid addition salt. The derivatives prepared by this process are also described. These compounds are useful as antibacterial agents.

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