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

YK Zhang, JJ Plattner, EE Easom, D Waterson, M Ge…

文献索引：Zhang, Yong-Kang; Plattner, Jacob J.; Easom, Eric E.; Waterson, David; Ge, Min; Li, Zhiya; Li, Lingchao; Jian, Yong Tetrahedron Letters, 2011 , vol. 52, # 30 p. 3909 - 3911

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被引用次数: 13

摘要

Abstract 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 IC 50= 26 nM against the malaria parasite Plasmodium falciparum.