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  • Title: Toward the Synthesis of Fluorinated Analogues of HCV NS3/4A Serine Protease Inhibitors Using Methyl α-Amino-β-fluoro-β-vinylcyclopropanecarboxylate as Key Intermediate.
    Author: Milanole G, Andriessen F, Lemonnier G, Sebban M, Coadou G, Couve-Bonnaire S, Bonfanti JF, Jubault P, Pannecoucke X.
    Journal: Org Lett; 2015 Jun 19; 17(12):2968-71. PubMed ID: 26053226.
    Abstract:
    Synthesis of fluorocyclopropyl building blocks, which constitute the core of various therapeutic agents against the hepatitis C virus, is described. The relevant methyl α-amino-β-fluoro-β-vinylcyclopropanecarboxylate has been used as a key intermediate for the total synthesis of a fluorinated analogue of Simeprevir (TMC 435), a HCV NS3/4A protease inhibitor.
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