WHERE R IS SELECTED FROM THE ROUP CONSISTING OF LOWERALKYL, LOWERALKENYL, ARYL, SUBSTITUTED ARYL, BENZYL, SUBSTITUTED BENZYL, AROXYALKYL, AND SUBSTITUTED AROXYALKYL; R1 IS HYDROGEN OR METHYL; R2 IS HYDROGEN OR LOWERAKNANOYL AND R3 IS HYDROGEN OR HYDROXYL SAID ERYTHROMYCIN DERIVATIVES BEING USEFUL FOR THIER ANTIBIOTIC ACTIVITY.
Abstract:
Covers 4''''-O-sulfonyl erythromycin-9-O-oxime derivatives falling within the following structural formula: WHERE R is selected from the group consisting of loweralkyl, loweralkenyl, aryl, substituted aryl, benzyl and substituted benzyl, R1 is hydrogen or methyl, R2 is hydrogen or loweralkanoyl, R3 is hydrogen or hydroxyl, and R4 is selected from the group consisting of loweralkyl, cycloalkyl, substituted cycloalkyl, aryl, substituted aryl, benzyl and substituted benzyl. These 9-O-oxime derivative compounds are useful as antibiotics.
Abstract:
1467296 Erythromycin derivatives ABBOTT LABORATORIES 1 May 1974 [4 May 1973] 19163/74 Heading C2C Novel erythromycin derivatives of the general formula wherein R is a C 1-6 alkyl, C 2-6 alkenyl, or optionally nuclear substituted aryl, benzyl or aroxyalkyl group, R 1 is a hydrogen atom or methyl group, R 2 is a hydrogen atom or C 1-6 alkanoyl group and R 3 is a hydrogen atom or hydroxyl group, provided that R 1 and R 3 are not simultaneously a hydrogen atom and the nuclear substituent is nitro, alkyl or halogen are prepared by reacting the corresponding compound in which the -OSO 2 R group is replaced by -OH with RSO 2 Cl (when R is vinyl in the product, R may be 2-bromoethyl in the starting material), followed optionally by hydrolysis or alcoholysis when R 2 is a C 1-6 alkanoyl group to give the corresponding product wherein R 2 is a hydrogen atom. Pharmaceutical compositions having antibiotic activity comprise, as active ingredient, an erythromycin derivative of the above general formula, together with an appropriate carrier.