ERYTHROMYCIN DERIVATIVE AND ITS PRODUCTION

PROBLEM TO BE SOLVED: To produce a new erythromycin derivative excellent in stability and useful for treatment of bacterial infection by oral administration. SOLUTION: This erythromycin derivative is 6-O-methylerythromycin A 9-hydrazone of formula I. The compound of formula I is obtained by reacting...

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Hauptverfasser:	JOSEPH KASPI, VLADIMIR NADAKA
Format:	Patent
Sprache:	eng
Schlagworte:	CHEMISTRY DERIVATIVES THEREOF HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY NUCLEIC ACIDS NUCLEOSIDES NUCLEOTIDES ORGANIC CHEMISTRY PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS SUGARS
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Beschreibung
Zusammenfassung:	PROBLEM TO BE SOLVED: To produce a new erythromycin derivative excellent in stability and useful for treatment of bacterial infection by oral administration. SOLUTION: This erythromycin derivative is 6-O-methylerythromycin A 9-hydrazone of formula I. The compound of formula I is obtained by reacting a compound of formula II [R1 is H or a 1-6C alkyl; R2 is a 1-6C alkyl or a (substituted) aryl; R1 and R2 may mutually be bound to form a 3-10C alkylene ring; R3 and R4 are each H or a substituted silyl] with hydrazine in a solvent such as an aqueous alcohol in the presence of an acid such as acetic acid and formic acid, and optionally deprotecting a silyl-protecting group.