| 摘要 |
Bromopenicillanate dioxides I (R=H, Br; R1=H, halogen, OAc; R2=H, ester gp.) were prepd. diazotizing 6beta-aminopenicillanate with equiv. nitrosating agent in the presence of 1-5 equiv. strong acid in the mixt. of H2O and org. solvent. Thus, 6beta-aminopenicillanic acid 1,1-dioxide in dil. H2SO4-MeCN was reacted with pyridine hydrobromide perbromide and NaNO2 to give I (R=H, Br; R1=R2=H) in 1:8 ratio and 78.2% total yield (I) inhibits betalactamase.
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