Improvement in synthesis of 3’-N-demethylazithromycin and its derivatives

【摘要】 3’-N-demethylazithromycin is an impurity in azithromycin drug. It is derived by demethylation of az- ithromycin,i. e. ,azithromycin loses a methyl group on the 3’-N position. In this study,bulk product was puri- fied with chromatographic separation. It was observed that 3’-N-demethylazithromycin was also a precursor of other impurities. Simultaneously,another derivative was synthesized,i. e. ,3’-N-demethyl-3’-N-formylazithro- mycin. Reaction conditions were optimized with the HPLC method and good-quality and high-yield derivative product was achieved. The structures of derivatives were identified by 1 H-NMR and MS.更多还原

【Abstract】 3’-N-demethylazithromycin is an impurity in azithromycin drug. It is derived by demethylation of az- ithromycin,i. e. ,azithromycin loses a methyl group on the 3’-N position. In this study,bulk product was puri- fied with chromatographic separation. It was observed that 3’-N-demethylazithromycin was also a precursor of other impurities. Simultaneously,another derivative was synthesized,i. e. ,3’-N-demethyl-3’-N-formylazithro- mycin. Reaction conditions were optimized with the HPLC method and good-quality and high-yield derivative product was achieved. The structures of derivatives were identified by 1 H-NMR and MS.更多还原