Breinbauer Rolf, Mentel Matthias
Institute of Organic Chemistry, Graz University of Technology, Graz, Austria.
Methods Mol Biol. 2009;572:73-80. doi: 10.1007/978-1-60761-244-5_5.
Solid Phase Organic Synthesis (SPOS) has become a powerful tool for the preparation of compound libraries used for screening efforts in Chemical Biology. While different types of screening libraries have become commercially available through several vendors, the elaboration of a hit compound in a screening campaign to a useful chemical probe still requires the preparation of a focused library. In this report, protocols are given which allow the synthesis of a focused compound library on solid phase by the diversification of a central scaffold using reliable functionalization reactions. Diversity elements can be introduced by attaching building blocks via amidation, esterification, reductive amination, and Suzuki cross-coupling.
固相有机合成（SPOS）已成为制备用于化学生物学筛选的化合物库的有力工具。虽然通过几家供应商已经可以商业获取不同类型的筛选库，但在筛选活动中将命中化合物精制为有用的化学探针仍需要制备一个聚焦库。在本报告中，给出了一些方案，这些方案允许通过使用可靠的官能团化反应使中心支架多样化，从而在固相上合成聚焦化合物库。可以通过酰胺化、酯化、还原胺化和铃木交叉偶联连接构建模块来引入多样性元素。
