A carbohydrate-derived trifunctional scaffold for DNA-encoded libraries

被引：4

作者：

Estevez, Amalia M. ^{[1
]}

Gruber, Felix ^{[2
]}

Satz, Alexander L. ^{[2
]}

Martin, Rainer E. ^{[2
]}

Wessel, Hans Peter ^{[1
]}

机构：

[1] Univ Aveiro, Dept Chem, P-3810193 Aveiro, Portugal

[2] F Hoffmann La Roche Ltd, Roche Innovat Ctr Basel, Roche Pharmaceut Res & Early Dev PRED, Med Chem, CH-4070 Basel, Switzerland

来源：

TETRAHEDRON-ASYMMETRY | 2017年 / 28卷 / 06期

关键词：

SMALL-MOLECULE LIBRARIES; CHEMICAL LIBRARIES; TECHNOLOGY ELT; DISCOVERY; POTENT; DERIVATIVES; INHIBITORS; SELECTION; SPACE;

D O I：

10.1016/j.tetasy.2017.04.007

中图分类号：

O61 [无机化学];

学科分类号：

070301 ; 081704 ;

摘要：

For the generation of DNA-encoded libraries, a central scaffold containing three exit vectors with defined chirality was devised starting from commercially available tri-O-acetyl-glucal. This scaffold may be connected to the DNA barcode at any of the three different exit vectors, thus making it a versatile approach as this readily leads to three different libraries. For one of the three possibilities, the compatibility with the DNA tag was demonstrated. The reactions include amide bond formation, Boc deprotection, urea formation, azide reduction and reductive alkylation. (C) 2017 Elsevier Ltd. All rights reserved.

引用

页码：837 / 842

页数：6

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