• DOI:10.1016/j.bmc.2015.06.035
Corpus ID: 25092621

One-pot synthesis of human metabolites of SAR548304 by fungal peroxygenases.

@article{Kiebist2015OnepotSO,
  title={One-pot synthesis of human metabolites of SAR548304 by fungal peroxygenases.},
  author={Jan Kiebist and W. Holla and J. Heidrich and Marzena Poraj-Kobielska and M. Sandvoss and Reiner Simonis and Glenn Gr{\"o}be and J. Atzrodt and M. Hofrichter and K. Scheibner},
  journal={Bioorganic & medicinal chemistry},
  year={2015},
  volume={23 15},
  pages={
          4324-32
        }
}

Jan Kiebist, W. Holla, +7 authors K. Scheibner

Published 2015

Chemistry, Medicine

Bioorganic & medicinal chemistry

Unspecific peroxygenases (UPOs, EC 1.11.2.1) have proved to be stable oxygen-transferring biocatalysts for H2O2-dependent transformation of pharmaceuticals. We have applied UPOs in a drug development program and consider the enzymatic approach in parallel to a conventional chemical synthesis of the human metabolites of the bile acid reabsorption inhibitor SAR548304. Chemical preparation of N,N-di-desmethyl metabolite was realized by a seven-step synthesis starting from a late precursor of… CONTINUE READING

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