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Concise Chemoenzymatic Total Synthesis of GE81112 B1 and Simplified Analogs Enable Elucidation of Its Key Pharmaco-phores

preprint
revised on 20.07.2020 and posted on 21.07.2020 by Christian Zwick, Max Sosa, Hans Renata
We report a chemoenzymatic total synthesis of GE81112 B1 that employs biocatalytic hydroxylation to prepare two of the key monomers of the target natural product. By pairing this strategy with traditional organic chemistry, we were able to synthesize GE81112 B1 in 11 steps. Following this strategy, six GE81112 analogs were synthesized, allowing for elucidation of its key pharmacophores.

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

USA

ORCID For Submitting Author

0000-0003-2468-2328

Declaration of Conflict of Interest

No conflict of interest

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