Molbank (Jun 2021)

2-Cyclopropyl-6-phenyl-2,3-dihydrothieno[3,2-<i>d</i>][1,3,2]diazaborinin-4(1<i>H</i>)-one

  • Romain Mustière,
  • Patrice Vanelle,
  • Nicolas Primas

DOI
https://doi.org/10.3390/M1221
Journal volume & issue
Vol. 2021, no. 2
p. M1221

Abstract

Read online

As part of our ongoing scaffold hopping work on antimalarial 2-aminothieno[3,2-d]pyrimidin-4-one scaffold, we explored the dihydrothieno[3,2-d][1,3,2]diazaborinin-4(1H)-one as a potential new antimalarial series. Using conditions found in the literature, we obtained 2-cyclopropyl-6-phenyl-2,3-dihydrothieno[3,2-d][1,3,2]diazaborinin-4(1H)-one with 93% yield through a simple treatment. It was then characterized by NMR (1H and 13C) and HRMS. Given the structure of this molecule, its aqueous stability was assessed to determine its suitability for biological tests. To our knowledge, this is the first dihydrothieno[3,2-d][1,3,2]diazaborinin-4(1H)-one described.

Keywords