| 摘要 |
<p>A new penicillin 6-(b -amino-b -phenylpropionamido) penicillanic acid, and its non-toxic salts, are prepared by coupling 6-amino-penicillanic acid or a salt thereof with an amino substituted b -amino-b -phenylpropionic acid, or a functional derivative thereof of formula <FORM:1057028/C2/1> where X is a protecting group for the amino radical and thereafter removing the protecting group to yield the desired penicillin. Coupling is by (a) acylation with acid halide, azide or anhydride of the said b -amino-b -phenylpropionic acid or a mixed anhydride thereof with another carboxylic acid, e.g. ethoxyformic acid, or (b) acylation with above reactants in the presence of a carbodiimide, e.g. dicyclohexyl-carbodiimide. The amino radical protecting group is of formula R.O.CO- where R is alkyl, benzyl, substituted benzyl, phenyl, substituted phenyl or trityl and may be removed by catalytic hydrogenation. The penicillin has similar acid stability to penicillin V and is active against penicillin V- or G-resistant microorganisms. It may be mixed with pharmaceutical diluents. Typical salts are the sodium, potassium, calcium, procaine or N,N1-dibenzylethylene diamine salts.</p> |
