Efficient synthesis is essential for antimalarial therapeutics. A four-step route has been established for the synthesis of 7-(2-carboxyethyl)-1,3-dihydro-1-hydroxy-2,1-benzoxaborole, which is a potent new class boron-containing antimalarial agent in preclinical development with IC50 = 26 nM against the malaria parasite Plasmodium falciparum.
Easom, E.E.; Ge, M.; Jian, Y.; Li, L.C.; Li, Z.Y.; Plattner, J.J.; Waterson, D.; Zhang, Y.K. An efficient synthesis for a new class antimalarial agent, 7-(2-carboxyethyl)-1,3-dihydro-1-hydroxy-2,1-benzoxaborole. Tetrahedron Letters (2011) 52 (30) 3909-3911. [DOI: 10.1016/j.tetlet.2011.05.088]