Solid-phase traceless synthesis of selected nitrogen-containing heterocyclic compounds.: The Encore technique for directed sorting of modular solid support

被引：14
作者：
Krchnák, V [1 ]
Smith, J [1 ]
Vágner, J [1 ]
机构：
[1] SIDDCO Inc, Tucson, AZ 85747 USA
来源：
COLLECTION OF CZECHOSLOVAK CHEMICAL COMMUNICATIONS | 2001年 / 66卷 / 07期
关键词：
heterocycles; solid-phase synthesis; combinatorial libraries; benzimidazoles; quinoxalines; benzylamine linkers;
D O I：
10.1135/cccc20011078
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
The acid lability of electron-rich N-benzylanilines has been exploited in a linker for the traceless solid-phase synthesis of benzimidazoles, 2-aminobenzimidazoles, quinoxalinones and tetrahydroquinoxalines. The target compound precursors were assembled on a solid-phase support derivatized with either a benzylamine or a benzhydrylamine linker. Exposure to an acidic reagent caused cleavage of the C(benzyl)-N(aniline) bond, releasing the product with only a hydrogen atom on the descending nitrogen. The Encore technique for directed sorting on SynPhase Lanterns has been developed and applied to combinatorial synthesis of generic drug discovery libraries.
引用
收藏
页码：1078 / 1106
页数：29
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