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Synlett 1998; 1998(3): 322-324
DOI: 10.1055/s-1998-1621
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Expeditious Synthesis of 4-(tert-Butylcarbonyl)-7α-methoxy-3-methyl-Δ3-cephem 1,1-Dioxide. Convenient Access to 7-Substituted Analogues

Marco Alpegiani* , Pierluigi Bissolino, Matteo D'Anello, Massimiliano Palladino, Ettore Perrone
  • *Pharmacia & Upjohn, 20014 Nerviano (Milano), Italy; E-mail: marco.alpegiani@eu.pnu.com
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Publication History

Publication Date:
31 December 2000 (online)

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A practical and efficient route leading to the synthesis of 4-(tert-butylcarbonyl)-7α-methoxy-3-methyl-Δ3-cephem 1,1-dioxide (2), a key-intermediate in the preparation of potent inhibitors of mammalian serine proteinases, is reported. The new synthetic pathway has allowed easy access to an array of 7-substituted cephem derivatives.

cephems - 1,1-dioxocephem tert-butyl ketones - 7-diazocephem - methoxylation - protease inhibitors

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