| 摘要 |
<p>Cephalosporins of the general formula <FORM:0982252/C2/1> wherein R1, taken alone, is -OH, C1-C8 acyloxy, or tertiary-amino; R2 is -OH when R1 is OH; R2 is -OH when R1 is C1-C8 acyloxy; R2 is -O- when R1 is tertiaryamino; R1 and R2, when taken together, are -O-; n is 0 or 1; R3 is C1-C6 alkylene: and R4 is a heteromonocyclic radical containing in the ring at least one atom of oxygen, nitrogen or sulphur, and the pharmaceutically acceptable salts, esters and amides thereof, such as 7 - b - (21 - furyl)propionamido -, 7 - (21 - furyl) acetamido -, 7 - (21 - thienyl)acetamido -, 7 - (y - 21 - thienyl - n - butyramido) -, 7 - (11-pyrazoleacetamido) -, and 7 - (N1 - pyrrylacetamido) - cephalosporanic acid, may be prepared by (A) acylating a compound having the bicyclic ring structure of cephalosporin C and having a general formula represented by one of <FORM:0982252/C2/2> wherein R11 is -OH or a C1-C8 acyloxy radical, and Am+ is a tertiary amino radical, with an acylating agent having at least one constituent radical of the general formula <FORM:0982252/C2/3> or (B) acylating a compound having the general formula <FORM:0982252/C2/4> with an acylating agent having at least one constituent radical of the general formula <FORM:0982252/C2/5> and heating the product with acidified water to form the corresponding heteromonocyclic acyl derivative of the nuclei of cephalosporin CC compounds, refluxing the product in solution with an excess of a tertiary amine corresponding to Am+ as defined above to form the corresponding heteromonocyclic derivative of the nuclei of cephalosporin CA compounds, or treating the product with citrus acetylesterase in a buffered aqueous medium to form the corresponding heteromonocyclic derivative of the nuclei of desacetylcephanosporin C compounds. A pharmaceutical composition comprises a cephalosporin of the first formula shown above and a pharmaceutical carrier. Specification 810,196 is referred to.</p> |
