红霉素衍生物的合成研究。3''-表红霉素A和(9S)-11-脱羟基-9-脱氧-9-羟基-11-氧代红霉素A的合成及抗菌活性。
Synthetic studies of erythromycin derivatives. Synthesis and antimicrobial activities of 3''-EPI-erythromycin A and (9S)-11-dehydroxy-9-deoxo-9-hydroxy-11- oxoerythromycin A.
作者信息
Nakata M, Tamai T, Miura Y, Kinoshita M, Tatsuta K
机构信息
Department of Applied Chemistry, Faculty of Science and Technology, Keio University, Yokohama, Japan.
出版信息
J Antibiot (Tokyo). 1993 May;46(5):813-26. doi: 10.7164/antibiotics.46.813.
PMID:8514636
Abstract
Two new derivatives, 3''-epi-erythromycin A (2) and (9S)-11-dehydroxy-9-deoxo-9-hydroxy-11-oxoerythromycin A (3), have been synthesized by using glycosylation with glycal (Ferrier rearrangement), bromomethoxylation and bis(tributyltin) oxide-bromine oxidation as the key steps. Their antimicrobial activities were compared with those of erythromycin A (1).
摘要
通过以烯丙基糖基化（费里尔重排）、溴甲氧基化和双（三丁基锡）氧化物-溴氧化为关键步骤，合成了两种新的衍生物，3''-表红霉素A（2）和（9S）-11-脱羟基-9-脱氧-9-羟基-11-氧代红霉素A（3）。将它们的抗菌活性与红霉素A（1）的抗菌活性进行了比较。
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