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Concise Chemoenzymatic Synthesis of Fasamycin A
preprintsubmitted on 04.03.2021, 21:27 and posted on 05.03.2021, 13:06 by Jian Li, Hans Renata
We report the development of a chemoenzymatic approach towards fasamycin A, a halogenated naphthacenoid that exhibits activities against methicillin-resistant Staphylococcus aureus and vancomycin-resistant Enterococcus faecalis. The synthesis was accomplished in a convergent manner: two fragments were combined together via Michael−Dieckmann condensation to afford a dimethylnaphthacenone system. Finally, an enzymatic halogenation was employed to introduce the requisite chlorine substituent of the natural product at a late stage.
Biocatalytic C -H Functionalization Logic in the Chemoenzymatic Synthesis of Therapeutic Natural Products
National Institute of General Medical SciencesFind out more...