| 摘要 |
<p>NEW MATERIAL:A compound shown by the formulaI(R is alkyl). EXAMPLE:11-O-Methylerythromycin A. USE:An antibacterial agent showing improved antibacterial activity in living body. PROCESS:For example, a compound (e.g., O,N-dibenzyloxycarbonyl-des-N-methyl- erythromycin A, etc.) shown by the formula II (Z is H or benzylcarbonyloxy) is reacted with an alkylating agent (e.g., methyl iodide, etc.) in the presence of a base such as sodium hydride, etc. so that the hydroxyl group at 11 position of erythronolide ring is alkylated, to give a compound shown by the formula III (R is alkyl), which is isolated and purified. The isolated compound is reduced catalytically, the protecting group Z is eliminated, and reduced catalytically in the presence of excess formaldehyde, so that it is N-methylated, to give a compound shown by the formulaI.</p> |
