| 摘要 |
<p>1417099 Penicillin-related amidines LEO PHARMACEUTICAL PRODUCTS Ltd A/S (LOVENS KEMISKE FABRIK PRODUKTIONSAKTIESELSKAB) 25 Jan 1974 [2 Feb 1973] 5414/73 Heading C2C The invention comprises a method for making compounds of Formula I() in which R 1 , R 2 and R 3 each represent an unsubstituted or substituted aliphatic hydrocarbon radical, a mono- or bicyclic carbocyclic aryl radical, an aralkyl radical, a cycloalkyl radical, a cycloalkyl-alkyl radical, a heterocyclic radical, or a heterocyclically substituted alkyl radical; R 3 further representing hydrogen; R 1 and R 2 together with the nitrogen atom represent a ring system; R 1 and R 3 together with the N-C atoms represent a ring system; and pharmaceutically acceptable, non-toxic salts thereof; in which a reactive derivative of a compound of Formula (II) where R 5 is O or S is reacted with a salt of 6- aminopenicillanic acid (or a mixture of the acid and a salt-forming compound) in a solvent at or below room temperature and the product is optionally converted into said non-toxic salt. Therapeutic compositions for parenteral administration comprise the above compounds (I).</p> |
