| 摘要 |
The invention relates to 6-(31-methyl-41-furazanacetamido) penicillanic acid of formula <FORM:1124920/C2/1> and non-toxic pharmaceutically acceptable salts thereof, e.g. sodium, calcium, aluminium, ammonium and amine salts. The compounds are prepared by acylating 6-aminopenicillanic acid, or a salt thereof, with an acylating derivative of an acid of formula <FORM:1124920/C2/2> 3-methyl-4-furazanacetic acid is prepared by (a) treating 3-methyl-4-furazancarbonyl chloride with diazomethane to form the diazoketone, (b) treating the diazoketone with benzyl alcohol and N,N1-dimethylaniline to form the benzyl ester of 3-methyl-4-furazanacetic acid, and (c) hydrolysing the benzyl ester with mineral acid. The starting material for (a) is produced by treating 3-methyl-4-furazancarboxylic acid with thionylchloride. The penicillins are effective against gram-positive and gram-negative bacteria and may be administered orally to man and animals, e.g. for the treatment of mastitis in cattle or as a nutritional supplement in animal feeds. The penicillins may be formulated into pharmaceutical compositions. |
