| 摘要 |
<p>1393348 Trifluoromethylmercaptoacetamidocephalosporins SMITHKLINE CORP 6 July 1973 [20 July 1972] 32261/73 Heading C2C Novel trifluoromethylmercaptoacetamidocephalosporins of the formula in which A is hydrogen, acetoxy, pyridinium, methoxy, methylthio or S-Het; Het is a 5 or 6 membered heterocyclic ring containing 1-4 hetero atoms selected from N, O and S and being unsubstituted or substituted with one or two groups selected from C 1-4 alkyl, C 1-4 alkoxy, C 1-4 alkylthio, C 3-4 cycloalkyl, halogen, hydroxy, allyl, methoxymethyl, mercapto, trifluoromethyl and NR 2 ; and R is hydrogen or C 1-6 alkyl, and pharmaceutically acceptable salts thereof, are prepared by acylation of the appropriate 7- aminocephalosporin with trifluoromethylmercaptoacetic acid. Trifluoromethylmercaptoacetic acid is prepared by treating iodoacetic acid with silver trifluoromethyl-mercaptan. N-Hydroxysuccinimidyl trifluoromethylmercaptoacetate is prepared by reacting trifluoromethylmercaptoacetic acid with N-hydroxysuccinimide. The 2,4-dinitrophenyl ester is similarly prepared. Pharmaceutical compositions having antibacterial activity comprise the above cephalosporins and a pharmaceutically acceptable carrier.</p> |
