An efficient synthesis for a new class antimalarial agent, 7-(2-carboxyethyl)-1,3-dihydro-1-hydroxy-2,1-benzoxaborole

18 Jul 2011

Yong-Kang Zhang, Jacob J. Plattner, Eric E. Easom, David Waterson, Min Ge, Zhiya Li, Lingchao Li, Yong Jian

Tetrahedron Letters

DOI:  10.1016/j.tetlet.2011.05.08


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 1 that is a potent new class boron-containing antimalarial agent in preclinical development with IC50 = 26 nM against the malaria parasite Plasmodium falciparum.

Read the full article on Science Direct.