Toward the Synthesis of Fluorinated Analogues of HCV NS3/4A Serine Protease Inhibitors Using Methyl α-Amino-β-fluoro-β-vinylcyclopropanecarboxylate as Key Intermediate - Archive ouverte HAL
Article Dans Une Revue Organic Letters Année : 2015

Toward the Synthesis of Fluorinated Analogues of HCV NS3/4A Serine Protease Inhibitors Using Methyl α-Amino-β-fluoro-β-vinylcyclopropanecarboxylate as Key Intermediate

Résumé

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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Dates et versions

hal-01179463 , version 1 (22-07-2015)

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Gaëlle Milanole, Floris Andriessen, Gérald Lemonnier, Muriel Sebban, Gaël Coadou, et al.. Toward the Synthesis of Fluorinated Analogues of HCV NS3/4A Serine Protease Inhibitors Using Methyl α-Amino-β-fluoro-β-vinylcyclopropanecarboxylate as Key Intermediate. Organic Letters, 2015, 17 (12), pp.2968-2971. ⟨10.1021/acs.orglett.5b01216⟩. ⟨hal-01179463⟩
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