摘要 |
PROBLEM TO BE SOLVED: To provide a quick and efficient method for producing 6-O-alkylerythromycin A by using a moderate and neutral reaction condition for suppressing the formation of undesirable byproducts. SOLUTION: This method for producing a 9-O-oximesilyl-6-O-alkyl erythromycin A derivative is provided by forming a 9-oximesilyl erythromycin A derivative by silylating a 9-oxime erythromycin A derivative, then reacting the 9-oximesilyl erythromycin A derivative with an alkylating agent and selectively alkylating at 6-oxygen. Further, the method for producing the 6-O-alkyl erythromycin A comprises the deoximation of the 9-O-oximesilyl-6-O-alkyl erythromycin A derivative. The 6-O-alkyl erythromycin A produced by the above method, e.g. clarythromycin is an important macrolide-based antibiotic. COPYRIGHT: (C)2007,JPO&INPIT
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