Benzoxaborole Building Blocks for Drug Discovery and Functional Group Conversion

Benzoxaborole Building Blocks for Drug Discovery and Functional Group Conversion

Benzoxaborole (D6273, A2559, D6272, D6277, D6275, D6270, D6271) is a boron-containing building block for drug discovery. This scaffold is found in pharmacologically active compounds with unique mechanisms of action, such as tavaborole (T3775), a leucyl t-RNA synthase inhibitor, and crisaborole, a PDE4 inhibitor¹,²). TCI offers a lineup of benzoxaboroles with various substituents on the benzene ring: amino (D6273 and A2559), carboxylic acid (D6272, D6270, D6271), and hydroxyl (D6277 and D6275), for functional group conversion reactions such as condensation and aromatic substitution³,⁴). With substituents at different ring positions, these building blocks allow further derivatization of the benzoxaborole core³,⁴).

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References

  1. Recent developments in the medicinal chemistry of single boron atom-containing compounds. S. Song, X. Liu, et al., Acta Pharm. Sin. B 2021, 11, 3035. doi:10.1016/j.apsb.2021.01.010
  2. The Boron Advantage: The Evolution and Diversification of Boron’s Applications in Medicinal Chemistry. K. Messner, B. Vuong, G. K. Tranmer, Pharmaceuticals 2022, 15, 264. doi:10.3390/ph15030264
  3. Design, Synthesis, and Structure−Activity Relationship of Trypanosoma brucei Leucyl-tRNA Synthetase Inhibitors as Antitrypanosomal Agents. D. Ding, H. Zhou, et al., J. Med. Chem. 2011, 54, 1276. doi:10.1021/jm101225g
  4. Discovery of Novel Benzoxaborole-Based Potent Antitrypanosomal Agents. D. Ding, J. J. Plattner, et al., ACS Med. Chem. Lett. 2010, 1, 165. doi:10.1021/ml100013s

Download TCI brochure Benzoxaboroles ― Boron-Containing Building Blocks for Drug Discovery (PDF)

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