5-o-desosaminylerythronolide a derivatives

C - Chemistry – Metallurgy – 07 – H

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C07H 17/08 (2006.01) C07H 17/00 (2006.01)

Patent

CA 2118489

Object: To provide novel macrolide antibiotics having a strong antibacterial activity. Constitution: 5-O-desosaminylerythronolide A derivatives represented by the formula: (see fig. I) [wherein -A~ is a group of -N(R3)- (wherein R3 is a hydrogen atom or an alkyl group having 1 - 3 carbon atoms) or a group represented by -N=, and R1 and R2 are each a hydrogen atom or an alkyl group having 1 - 3 carbon atoms] which is a tricyclic carbamate of 5-O-desosaminylerythronolide A derivative having a ketone at the 3-position, being substituted by a methoxy group at the 6-position, and a pharmaceutically acceptable acid addition salt thereof; and a compound represented by the formula: (see fig. II) (wherein R4 is an acetyl group or a propionyl group) which is an intermediate useful for the preparation of the 3-ketone forms of 5-O-desosaminylerythronolide A derivatives.

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