ERYTHROMYCIN A DERIVATIVE AND ITS PRODUCTION
PROBLEM TO BE SOLVED: To obtain an erythromycin A derivative useful as an intermediate for producing an antibiotic medicine 6-O-methylerythromycin A by protecting the 9-position of erythromycin A and selectively methylating the hydroxyl group at the 6-position. SOLUTION: This new erythromycin deriva...
Gespeichert in:
Hauptverfasser: | , |
---|---|
Format: | Patent |
Sprache: | eng |
Schlagworte: | |
Online-Zugang: | Volltext bestellen |
Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
Zusammenfassung: | PROBLEM TO BE SOLVED: To obtain an erythromycin A derivative useful as an intermediate for producing an antibiotic medicine 6-O-methylerythromycin A by protecting the 9-position of erythromycin A and selectively methylating the hydroxyl group at the 6-position. SOLUTION: This new erythromycin derivative is shown by formula I [R1 is H or a 1-6C alkyl; R2 is a 1-6C alkyl or a (substituted) alkyl; R1 and R7 are bonded to form a 3-10C alkylene ring or the like; R4 is H or a substituted silyl group] and is usefulas an intermediate for producing an antibiotic medicine 6-O-methylerythromycin A (clarithromycin), etc. This compound is obtained by converting erythromycin A into erythromycin A 9-hydrazone, converting the hydrazone into an erythromycin A 9-azine derivative of formula II, protecting the hydroxyl groups at the 2'- and the 4'-positions by silylation and methylating the hydroxyl group at the 6-position of the resultant substance. |
---|