| 摘要 |
1389540 Derivatives of α-aminocephalosporins BRISTOL-MYERS CO 20 Nov 1972 [3 Dec 1971] 56257/71 Heading C2C Novel α-aminocephalosporin derivatives having the Formula III or (IV) and acid addition salts thereof, wherein R is cyclohexadienyl, 2- or 3-thienyl, phenyl, or phenyl substituted by one or more groups selected from halo, hydroxy, C 1-6 alkyl, C 1-6 alkanoyl, C 1-6 alkanoyloxy, C 1-6 alkoxy, C 1-6 alkanoylamino, C 1-6 alkylmercapto, nitro, trifluoromethyl, and amino; and A is a cephem moiety of formula in which R<SP>1</SP> is hydrogen or a salt-forming ion and X is hydrogen or C 1-6 alkanoyloxy; are prepared by reacting acetaldehyde with an α-aminocephalosporin compound of Formula (I) or an acid addition salt thereof wherein A and R are as defined above. The compound (III) is produced by carrying out the reaction in a substantially anhydrous medium in which the products is insoluble, such as acetone or isopropanol. In a medium which is a solvent for the product, e.g. methylene chloride, and preferably contains water, the cyclic compound (IV) is produced. The products (III) and IV and their salts have antibiotic activity, and may be admixed with a pharmaceutically acceptable carrier to provide antibiotic pharmaceutical compositions. |
