Synthesis of novel 6,11-O-bridged bicyclic ketolides via a palladium-catalyzed bis-allylation |
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Authors: | Wang Guoqiang Niu Deqiang Qiu Yao-Ling Phan Ly Tam Chen Zhigang Polemeropoulos Alexander Or Yat Sun |
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Institution: | Enanta Pharmaceuticals, Inc., 500 Arsenal Street, Watertown, MA 02472, USA. wang@enanta.com |
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Abstract: | A bridging chemistry process was developed to form an ether bridge between 6-O and 11-O of erythromycin A via a tandem or stepwise palladium-catalyzed bis-pi-allylation. By applying this bridging process, new 6,11-O-bridged bicyclic ketolides (BBKs) were synthesized. These BBKs showed good antibacterial activities against the macrolide-susceptible strains as well as mef-resistant strains and served as a good core for further modifications to study the structure-activity relationship (SAR) and to overcome bacterial resistance. reaction: see text] |
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