| 摘要 |
<p>Indoles or indole derivatives which are coupled via the 4, 5, 6 or 7 position and which are of the general formula I, <IMAGE> in which D-A-O- is located in the 4, 5, 6 or 7 position, and where R1, R2 and R3 each denote H or any other group which does not affect the subsequent steps, because they are, where appropriate, protected with protecting groups which are known per se, or two or all the substituents R1, R2 and R3, together with the atoms to which they are linked, form a cyclic or heterocyclic system, A is a coupling residue, and D is a group of the formula Y-X-D' containing a nucleophilic radical where X is a direct linkage or a straight-chain or branched, saturated or unsaturated hydrocarbon group which has 1-9 carbon atoms and which is substituted one or more times, D' is NH-, -S-, -O- or -O- Ph-, where Ph denotes phenyl, and Y is a carboxylic acid group or an activated ester group of this acid group or Y is an alcohol group or a tosylate or tresylate derivative of this alcohol group, or is temporarily introduced as part of a leaving group. The said derivatives of the abovementioned formula I can be used when preparing biologically active indole-carrier conjugates.</p> |
