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Concise Chemoenzymatic Synthesis of Fasamycin A

preprint
submitted 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.

Funding

Biocatalytic C -H Functionalization Logic in the Chemoenzymatic Synthesis of Therapeutic Natural Products

National Institute of General Medical Sciences

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History

Email Address of Submitting Author

hrenata@scripps.edu

Institution

The Scripps Research Institute

Country

United States

ORCID For Submitting Author

0000-0003-2468-2328

Declaration of Conflict of Interest

No conflict of interest

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