| 摘要 |
<p>Disclosed are 2-aza-substituted 1-carbadethiapen-2-em-3-carboxylic acids I, where the generic 2-aza group includes azido, acylamino, amino, alkylamino, dialkylamino, triazolyl, triazolinyl, aziridinyl, and their pharmaceutically acceptable salt, ester, anhydride and amide derivatives which are useful as antibiotics. Also disclosed are processes for the preparation of I from the known, appropriately substituted bicyclic keto ester II via the 2-azido central intermediate III: <CHEM> <CHEM> wherein R<1><6> is H or CH3, preferably beta-methyl; R<6>, and R<7> are independently hydrogen, linear, branched or cyclic C1-C5alkyl, which can be substituted with fluoro, hydroxy, protected hydroxy, sulfoxy, amino, protected amino, wherein R<6> and R<7> taken together can also be C2-C4 alkylidene, similarly substituted; with the proviso that both R<6> and R<7> are not unsubstituted alkyl, R<1> and R<2> are, inter alia, hydrogen, alkyl, acyl, and can be joined to form a ring comprising 3 to 7 atoms; R<a> is hydrogen, a salt cation, a removable protecting group, or a pharmaceutically acceptable ester moiety. Also disclosed are pharmaceutical compositions comprising such compounds.</p> |
