Novel Preparation of 1,1-Dioxo-7α-methoxy-3-methyl-Δ3-cephem-4-yl Aryl Ketones

Marco Alpegiani; Pierluigi Bissolino; Matteo D'Anello; Ettore Perrone

doi:10.1055/s-1998-1620

Synlett 1998; 1998(3): 319-321
DOI: 10.1055/s-1998-1620

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Novel Preparation of 1,1-Dioxo-7α-methoxy-3-methyl-Δ³-cephem-4-yl Aryl Ketones

Marco Alpegiani^* , Pierluigi Bissolino, Matteo D'Anello, Ettore Perrone

^*Pharmacia & Upjohn, 20014 Nerviano (Milano), Italy; E-mail: marco.alpegiani@eu.pnu.com

Abstract

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1,1-Dioxo-7α-methoxy-3-methyl-Δ³-cephem-4-yl phenyl ketone, a valuable precursor of potent HLE inhibitors, was obtained in an efficient way starting from 7α-methoxy-3-methyl-Δ³-cephem-4-carboxylic acid. By employing the same methodology a variety of 1,1-dioxocephem-4-yl aryl ketones were prepared.

cephems - 1,1-dioxocephem aryl ketones - acylation - decarboxylation - protease inhibitors

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