C-20- and c-23-modified macrolide derivatives

Details C-20- and c-23-modified macrolide derivatives C-20- and c-23-modified macrolide derivatives

C - Chemistry, Metallurgy

07

H

260/230.35

C07H 17/08 (2006.01) A23K 1/17 (2006.01)

Patent

CA 1236830

ABSTRACT OF THE DISCLOSURE Described herein are novel C-20 and C-23 modified derivatives of tylosin and tylosin-like macro- lides having the following formula: Image (I) wherein R is hydrogen or a halo, cyano, hydroxy, alkoxy, aryloxy, azido, amino, amido or -SR5 group, where R5 is a C1-C4 alkyl, cyclohexyl, aryl or heteroaryl group; R1 is hydrogen, hydroxy, halo, -OAr, -O- tetrahydrofuranyl, -O-tetrahydropyranyl, -SR5 (as defined above), azido, amino, or amido; R2 is hydrogen, or an optionally substituted alkanoyl, benzoyl, phenylacetyl or phenylpropionyl group' and R3 is hydrogen, hydroxyl, or an optionally substituted C1-C5 alkanoyloxy, benzoyloxy, phenylacetoxy or phenyl propionyloxy group, or a mycarosyloxy group, and salts thereof. These compounds - ii - are useful as antibiotics and/or as intermediates for the preparation of antibiotics.

448380

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