摘要
A series of novel acylide derivatives have been synthesized from clarithromyc｜n A via a tacile procedure. The C-3 modifications involved replacing the natural C-3 cladinosyl group in clarithromycin core with different aryl-piperzine sidechain via chemical synthesis, Meanwhile a distinctive intermediate with 10,11-epoxy moiety was obtained, The structure and stereochemistry of this novel structure were confirmed via NMR and X-ray crystallography. Potential anti-bacterial activities against both Grampositive and Gram-negative bacteria were reported. Because of existence of C10,11-epoxide, these derivatives can be used as intermediates for further structural modification.
A series of novel acylide derivatives have been synthesized from clarithromyc｜n A via a tacile procedure. The C-3 modifications involved replacing the natural C-3 cladinosyl group in clarithromycin core with different aryl-piperzine sidechain via chemical synthesis, Meanwhile a distinctive intermediate with 10,11-epoxy moiety was obtained, The structure and stereochemistry of this novel structure were confirmed via NMR and X-ray crystallography. Potential anti-bacterial activities against both Grampositive and Gram-negative bacteria were reported. Because of existence of C10,11-epoxide, these derivatives can be used as intermediates for further structural modification.
基金
supported by Jiangsu Hengrui Pharmaceutical Company.The X-ray crystallography was performed at Shanghai Institute of Organic Chemistry,China Academy of Science
