The stereoselective synthesis of novel macrolide antibacterial agents via an intramolecular 1,3-dipolar cycloaddition of azomethine ylide |
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| Authors: | Yu Gui Gu Xiaolin Zhang Richard F Clark Stevan W Djuric Zhenkun Ma |
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| Institution: | Infectious Disease Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 200 Abbott Park Road, Abbott Park, IL 60064, USA |
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| Abstract: | An intramolecular 1,3-dipolar cycloaddition of azomethine ylide, generated in situ via the reaction of C12-glycinate derivative of macrolide with formaldehyde, provided a novel tricyclic macrolide. The high stereoselectivity of this 2+3] reaction was achieved by introducing a suitable directing group at C-6 position of macrolide. |
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| Keywords: | Macrolide Ketolide Azomethine ylide |
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