4"-N-(Substituted)-apramycin antibiotic derivatives and intermediates therefor
AssigneeEli Lilly and Company
InventorHerbert A. Kirst
Life of this patent
Estimating the term…
Abstract
Apramycin derivatives substituted at the 4"-amino group with a variety of substituents are broad spectrum antibiotics. Also claimed are intermediates in the synthesis of these apramycin derivatives.
Claims14
A compound of the formula ##STR8## wherein R.sub.1 is C.sub.2 to C.sub.4 -alkyl, C.sub.1 to C.sub.4 -acyl, benzyl, methoxybenzyl, halobenzyl, .gamma.-amino-.alpha.-hydroxybutyryl, .beta.-amino-.alpha.-hydroxypropionyl, glycyl, 4-amino-2-hydroxybutyl, 3-amino-2-hydroxypropyl or 2-aminoetyl;
- and the pharmaceutically acceptable acid addition salts thereof.
A compound of the formula ##STR9## wherein R.sub.2 is C.sub.1 to C.sub.4 -acyl, .gamma.-phthalimido-.alpha.-hydroxybutyryl, .beta.-phthalimido-.alpha.-hydroxypropionyl or N-phthalimidoglycyl;
- R.sub.3 is benzyloxycarbonyl and
- R.sub.4 and R.sub.4 ' are each methyl, or, taken together form a cyclohexyl ring.
A compound of the formula ##STR10## wherein R.sub.5 is C.sub.1 -C.sub.4 -acyl, .gamma.-phthaliido-.alpha.-hydroxybutyryl, .beta.-phthalimido-.alpha.-hydrxypropionyl or N-phthalimidoglycyl;
- and R.sub.6 is benzyloxycarbonyl.
A compound of the formula ##STR11## wherein R.sub.7 is .gamma.-phthalimido-.alpha.-hydroxybutyryl, .beta.-phthalimido-.alpha.-hydroxypropionyl or N-phthalimidoglycyl.
Dependencies are inferred from the claim text.