Regioselectivity of thiouracil alkylation: Application to optimization of Darapladib synthesis

Guibbal, F; Benard, S; Patche, J; Meneyrol, V; Couprie, J; Yong-Sang, J; Meilhac, O; Jestin, E

Meilhac, O (reprint author), Univ La Reunion, INSERM, UMR Diabet Atherothrombose Therapies Reunion Ocea, St Denis, Reunion, France.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2018; 28 (4): 787

Abstract

Darapladib is one of the most potent Lp-PLA(2) (Lipoprotein-associated phospholipase A(2)) inhibitor with an IC50 of 0.25 nM. We demonstrate that a cr......

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