4.4 Article

Continuous-Flow Preparation of Benzotropolones: Combined Batch and Flow Synthesis of Epigenetic Modulators of the (JmjC)-Containing Domain

Journal

CHEMISTRYSELECT
Volume 6, Issue 39, Pages 10717-10721

Publisher

WILEY-V C H VERLAG GMBH
DOI: 10.1002/slct.202102457

Keywords

benzotropolones; continuous flow; enzymes; epigenetics; natural products

Funding

  1. MINECO [PID2019-107855RB-I00]
  2. Xunta de Galicia (DXPCTSUG) [GRC ED431 C 2017/61]
  3. Xunta de Galicia [ED-431G/02-FEDER]
  4. University of Vigo (Programa Retencion de Talento)
  5. Universidade de Vigo/CISUG

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A continuous flow synthetic protocol was described for the preparation of benzotropolones, and their derivatization to yield an inhibitor of (JmjC)-containing domain enzymes. The procedure proved to be efficient and reproducible, paving the way for the preparation of larger amounts of the product for more extensive biological studies.
A continuous flow synthetic protocol for the preparation of benzotropolones, and further derivatization to yield a recently described inhibitor of (JmjC)-containing domain enzymes is described. Our procedure renders the desired compound in an efficient and reproducible manner and paves the way towards the preparation of higher amounts of the product, needed for more extensive biological studies.

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