Suchý Mojmír, Li Alex X, Bartha Robert, Hudson Robert H E
Department of Chemistry, The University of Western Ontario, London, ON, Canada N6A 5B7.
Org Biomol Chem. 2008 Oct 7;6(19):3588-96. doi: 10.1039/b808282k. Epub 2008 Jul 11.
Several approaches towards asymmetrically derivatized peptide-decorated cyclens that yield lanthanide metal chelators, in which three of the nitrogen atoms of cyclen share a common substituent and the fourth nitrogen atom is differentially substituted, have been evaluated. The most effective route consisted of selective monoalkylation followed by peralkylation with a second different electrophile. The unique substituent also possessed a masked sulfanyl group that was suitable for subsequent chemoselective conjugation chemistry.
已对几种制备镧系金属螯合剂的方法进行了评估，这些方法用于制备不对称衍生化的肽修饰环糊精，其中环糊精的三个氮原子共享一个共同取代基，第四个氮原子被不同地取代。最有效的途径包括选择性单烷基化，然后用第二种不同的亲电试剂进行全烷基化。独特的取代基还具有一个掩蔽的硫烷基，适用于后续的化学选择性共轭化学。
