Tetrahedron

An efficient synthesis of Ecopladib

W Li, J Li, D DeVincentis, TS Mansour

Index: Li, Wei; Li, Jianchang; DeVincentis, Dianne; Mansour, Tarek S. Tetrahedron, 2008 , vol. 64, # 34 p. 7871 - 7876

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Citation Number: 3

Abstract

An efficient synthesis of Ecopladib, an indole inhibitor of cytosolic phospholipase A2α, is described. A new reaction involving indole C3 reductive alkylation using an acetal in the absence of water and a novel transformation of the C2 methyl to an aldehyde via dimethyl sulfoxide-mediated oxygen-transfer reaction are used in the present synthesis, which dramatically increased the synthetic efficiency.