Tetrahedron

Synthesis of mono-and di-substituted 2, 4, 5-trifluorobenzoic acid synthons, key precursors for biologically active 6-fluoroquinolones

G Anquetin, J Greiner, P Vierling

Index: Anquetin, Guillaume; Greiner, Jacques; Vierling, Pierre Tetrahedron, 2005 , vol. 61, # 35 p. 8394 - 8404

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Citation Number: 11

Abstract

In the search for new potent antiparasitical fluoroquinolones, a QSAR analysis by molecular connectivity led to the design of R5 (Me or Et)/R8 (MeO, Me or Et)-substituted analogs of the most powerful antibacterial or antiparasitical fluoroquinolones known so far. Unfortunately, the synthetic schemes that were elaborated in literature for 3-and 3, 6-di-substituted 2, 4, 5- trifluorobenzoic acids, the key precursors of the target R5/R8-substituted 6- ...