| 摘要 |
<p>New bicyclic compounds of the general formula (I), <IMAGE> wherein Y<1> and Y<2> represent a removable carbonyl protecting group, and Q is a C1-5 alkyl group or a substituted benzyl group, are prepared, e.g. in the way that leaving group X of a compound having the general formula (V), <IMAGE> wherein X is a selectively removable esterifying group, is removed, the carboxy group of the resulting new compound of the general formula (IV> <IMAGE> is activated and reacted then with a salt of a malonic acid hemiester, wherein the alcohol component is a C1-5 aliphatic alcohol or a substituted benzyl alcohol, the resulting new compound of the general formula (III> <IMAGE> is reacted with a sulfonic azide in the presence of a tertiary amine, and the resulting new compound of the general formula (II> <IMAGE> is subjected to ring closure. The compounds of the general formula (I) are pharmacologically active as beta -lactamase inhibitors or can be converted into pharmacologically active thienamycin derivatives.</p> |
