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红霉素A是一种重要的大环内酯抗生素.在大量红霉素的化学修饰研究中,除了红霉素B的11-氧-烷基取代(12-脱氧红霉素A)之外,没有报道过红霉素A的氧-烷基取代.本文作者叙述氧-甲基衍生物6-氧-甲基红霉素A和6,11-双-氧-甲基红霉素A的制备和抗细菌活性.2’-氧-3’-氮-双(苄氧基碳酰)-氮-去甲基红霉素A用CH_3I(8克当量)和NaH(1.2克当量)在二甲基亚砜:四氢呋喃(1:1)冰浴冷却30分钟甲基化.所获得混合物经硅胶柱层析,用醋酸乙酯:正己烷(1:2)为洗脱剂,洗
Erythromycin A is an important macrolide antibiotic.In addition to erythromycin B’s 11-oxo-alkyl substitution (12-deoxy erythromycin A) in a number of erythromycin chemical modification studies , No oxo-alkyl substitution of erythromycin A has been reported herein.The authors describe the use of the oxy-methyl derivatives 6-oxy-methylerythromycin A and 6,11-bis-oxy-methylerythromycin A Preparation and Antibacterial Activity 2’-O-3’-Nitrosobis (benzyloxycarbonyl) -nitroerythromycin A was treated with CH_3I (8 equivalents) and NaH Methyl sulfoxide: tetrahydrofuran (1: 1) was cooled in an ice bath for 30 minutes for methylation.The resulting mixture was purified by silica gel column chromatography using ethyl acetate: n-hexane (1: 2)