Laboratory for Organic and Biomimetic Chemistry, Department of Organic Chemistry, Faculty of Sciences, Ghent University, B-9000 Ghent, Belgium.
Molecules. 2011 Dec 7;16(12):10168-86. doi: 10.3390/molecules161210168.
We present three versatile solid-supported scaffold building blocks based on the (deoxy)cholic acid framework and decorated with handles for further derivatization by modern ligation techniques such as click chemistry, Staudinger ligation or native chemical ligation. Straightforward procedures are presented for the synthesis and analysis of the steroid constructs. These building blocks offer a new, facile and shorter access route to bile acid-peptide conjugates on solid-phase with emphasis on heterodipodal conjugates with defined spatial arrangements. As such, we provide versatile new synthons to the toolbox for bile acid decoration.
我们提出了三种基于（去氧）胆酸骨架的多功能固相支撑支架构建块，并通过现代连接技术（如点击化学、斯塔德勒连接或天然化学连接）进一步衍生化进行修饰。为甾体结构的合成和分析提供了简单的程序。这些构建块为固相上的胆酸-肽缀合物提供了一种新的、简单的和更短的途径，重点是具有明确定位排列的异双足缀合物。因此，我们为胆酸修饰工具箱提供了多功能的新合成子。
