| 摘要 |
PURPOSE:To obtain the titled compound useful as an antibacterial agent, with simple procedure in high yield, by using a specific protected des-N- methylerythromycin derivative as a starting raw material and contacting the derivative with a platinum-group metal compound in the presence of formic acid, thereby eliminating the protecting group from the derivative. CONSTITUTION:The protected des-N-methylerythromycin derivative of formula I (R1 is H or OH; R2 and R4 are H or lower alkyl; R3 is lower alkyl; R5-R7 are 2-alkenyl-type residue) used as a starting raw material is made to contact with a platinum-group metal compound catalyst in the presence of formic acid (salt) (preferably organic amine salt of formic acid, such as diethylamine formate) preferably at 50-150 deg.C usually for 5min-24hr. The deprotection reaction takes place to give the objective compound of formula II. Preferably, a bivalent organic Pd compound such as palladium acetate is used as the above platinum-group metal compound catalyst in combination with a ligand such as triphenylphosphine, etc. |
