C - Chemistry – Metallurgy – 07 – H
Patent
C - Chemistry, Metallurgy
07
H
260/230.56
C07H 15/22 (2006.01) C07H 15/234 (2006.01)
Patent
CA 1046512
ABSTRACT OF THE DISCLOSURE The disclosure describes a process for the preparation of 1-N-substituted derivatives of the 4,6-di-(aminoglycosyl)- 1,3-diaminocyclitols gentamicin A, gentamicin B, gentamicin B1, gentamicin C1, gentamicin C1a, gentamicin C2, gentamicin C2a, gentamicin X2, sisomicin, verdamicin, Antibiotic G-418, Antibiotic 66-40B, Antibiotic 66-40D, Antibiotic JI-20A, Antibiotic JI-20B and Antibiotic G-52. The 1-N-substituent is designated X, and represents S-3-amino-2-hydroxypropionyl or S-4-amino-2-hydroxybutyryl with the proviso that, in case of gentamicin C1, gentamicin C1a and gentamicin C2, X is S-3- amino-2-hydroxypropionyl. The process also produces the pharmaceutically acceptable acid addition salts of these derivatives. One of the above named 4,6-di-(aminoglycosyl)- 1,3-diaminocyclitols which may have amino-protecting groups at any position other than position 1 is treated with an acid of the formula HO - X' wherein X' is a group as defined for X above, wherein the amino group and/or the hydroxy group may be protected, in the presence of a carbodiimide, or with a reactive derivative of the above acid, all protecting groups present in the molecule are removed and the derivative as such or as a pharmaceutically acceptable acid addition salt is isolated. Derivatives produced by this process are also described. The compounds possess broad spectrum antibacterial activity.
218335
Scherico Ltd.
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