Chen J K, Weith H L, Grewal R S, Wang G, Cushman M
Department of Medicinal Chemistry, Purdue University, West Lafayette, Indiana 47907, USA.
Bioconjug Chem. 1995 Jul-Aug;6(4):473-82. doi: 10.1021/bc00034a018.
Four benzophenanthridine phosphoramidite reagents have been prepared in which the linker chain between the benzophenanthridine and the phosphoramidite moiety is attached to C-2, C-6, C-9, and C-12 of the benzophenanthridine ring system. These benzophenanthridine phosphoramidites should prove to be useful in the syntheses of antisense oligonucleotide-intercalator conjugates in which the linker chain is attached to various regions of the benzophenanthridine intercalator. One of the new benzophenanthridine phosphoramidite reagents was used to prepare an antisense oligonucleotide-intercalator conjugate in which the oligonucleotide TCAGTGGTp was connected at its 5'-hydroxyl group through a linker chain to the C-2 hydroxyl group of a benzophenanthridine.
已制备了四种苯并菲啶亚磷酰胺试剂，其中苯并菲啶与亚磷酰胺部分之间的连接链连接到苯并菲啶环系的C-2、C-6、C-9和C-12位。这些苯并菲啶亚磷酰胺在反义寡核苷酸-嵌入剂缀合物的合成中应会证明是有用的，其中连接链连接到苯并菲啶嵌入剂的各个区域。其中一种新的苯并菲啶亚磷酰胺试剂用于制备反义寡核苷酸-嵌入剂缀合物，其中寡核苷酸TCAGTGGTp在其5'-羟基处通过连接链连接到苯并菲啶的C-2羟基上。
