Synthesis of .DELTA.3-1-methylene-1-carbacephems

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Abstract
The total synthesis of (.+-.)-1-methylene-2,2-dimethyl-7-amino-1-carbacephem-4-carboxylic acid (1) is described. The reaction scheme was essentially that described by Christensen et al. for the synthesis of (.+-.)-1-carbacephems. In vitro antibacterial activities of the 7-phenoxyacetyl and 7-D-.alpha.-phenylglycyl derivatives of 1 were compared with those of 7-(phenoxyacetamido)desacetoxycephalosporanic acid and cefalexin. Derivatives of 1 were 2-4 times less active against most of the sensitive organisms than the corresponding 7-aminodesacetoxycephalosporanic acid analogues. The activity of the 7-D-.alpha.-phenylglycyl derivative of 1 however was about 20 times lower than that of cefalexin when measured against Staphylococcus aureus ATCC 6538P.

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