PROCESS FOR PREPARING 6-AMINOALKYL-PENICILLANIC AICD 1,1-DIOXIDES AND DERIVATIVES AS BETALACTAMASE INHIBITORS

摘要

The title compds. I and II [ R=H; n=1; Q=benzyl, o-, m-, phydroxybenzyl, penethyl, 2-, 3-, 4-picolyl; R1=H, ester! were prepd. Thus, 108.73g benzyl-6,6-dibromo-penicillanate in 600 ml THF (-78≰C) was reacted with 83.5 ml 2.9 M-methylmagnesium in ether soln., mixed with 27 g benzyloxycarboxy amido methyl acetate in 200 ml THF for 10 min., and treated with 14.52 ml acetic acid to give 113 g benzyl-6-α-bromo-6-β-(benzyloxycarbonyl-amino methyl) penicillanate.