| 摘要 |
<p>The invention relates to a method of preparing a diaminedithiol chelating agent by reacting a cyclic diamine disulfide with a thiol compound as a reducing agent, said thiol compound being selected from the group consisting of dithiothreitol, dithioerythritol, thioglycol, cysteine, N-acetylcysteine, glutathione, alpha -mercaptopropionylglycine, 4-mercaptopyridine, 2, 3-dimercapto-1-propanol, 1,4-dimercaptobutane and 1,3-dimercaptopropane. The invention further relates to a new N2S2-compound having general formula (III), wherein Z, Z1, Z2 and Z3 are equal or different and represent methylene groups, if desired substituted with one or two C1-C4 alkyl group(s), or carbonyl groups; R2, R3, R4 and R5 are equal or different and represent C1-C4 alkyl groups; R7 is a hydrogen atom or a C1-C16 hydrocarbyl group, if desired substituted with a pharmaceutically acceptable target specific group, derived from a compound selected from the group consisting of a protein or proteinaceous substance, a receptor binding agent and an amino compound, or with a group permitting derivatization to a target specific group, said group permitting derivatization being selected from the group consisting of a halogen atom, an aldehyde group, a carboxy group and an activated ester group; R8 is a hydrogen atom or a C1-C16 hydrocarbyl group, if desired substituted with said pharmaceutically acceptable target specific group or with said group permitting derivatization to a target specific group; R9 is a hydrogen atom or a C1-C4 alkyl group; and Y is a hydrogen atom or a suitable protective group; or a salt of this compound with a mineral or organic acid.</p> |
