| 摘要 |
<p>1438872 7 - [# - Aminoacylamino] - 3 - substituted - 3 - cephem-4 - carboxylic acid derivatives FUJISAWA PHARMACEUTICAL CO Ltd 31 Aug 1973 [17 Nov 1972 14 Feb 1973] 41218/73 Heading C2C Novel cephalosporamic acid derivatives have the formula wherein R 1 is hydrogen lower alkyl, lower alkenyl, aryl or a heterocyclic group, R 2 is hydrogen or lower alkyl or R 1 and R 2 mean, taken together with the adjacent carbon atom, cycloalkyl or cycloalkenyl, R 3 is hydrogen, lower alkylthio or a heterocyclic thio group but excluding 5-methyl-1,3,4-thio diazol-2-ylthio when R 1 and R 2 taken together with the adjacent carbon atom are cyclohexyl and M is hydrogen, and M is hydrogen or a non-toxic, pharmaceutically acceptable cation. These derivatives may be prepared by acylating 7- amino - 3 - substituted - 3 - cephem - 4 - carboxylic acids of the formula with a #-amino aliphatic carboxylic acid derivative of the formula wherein X is protected amino, and if necessary removing the protective group of the amino radical. In the instance wherein R 3 is lower alkylthio or a heterocyclic-thio group, the derivatives may be prepared by reacting 7-acylated aminocephalosporacic acids with nucleophiles of formula R 3 -H and then if necessary, removing the protective groups of the amino radical. Further, when R 3 is hydrogen, the derivatives may be prepared by reducing 7-acylated amino cephalosporanic acids, and then, if necessary, removing a protective group on the amino radical. 1 - Aminocyclohexane - 1 - acetyl chloride is prepared by reacting the free acid with thionylchloride. The derivatives may be used in the form of a pharmaceutical preparation for therapeutic administration.</p> |
