Andrews Stephen P, Jönsson Daniel, Warrington Brian H, Ladlow Mark
GlaxoSmithKline Cambridge Technology Centre, University Chemical Laboratory, Lensfield Road, Cambridge, CB2 1EW, UK.
Comb Chem High Throughput Screen. 2004 Mar;7(2):161-76. doi: 10.2174/138620704773120847.
The automated polymer-assisted solution phase (PASP) synthesis of a 72 member library of 2-alkylthio-benzimidazoles 16 and benzimidazolin-2-ones 17 using commercially available robotic workstations is described. By incorporating both automated aqueous work-ups, in-line scavenging and 'catch and release' protocols the desired compounds were obtained directly in good yields and excellent purities without the need for conventional chromatographic purification. The synthesis described demonstrates how both manual and automated equipment may be utilised together to provide a versatile approach that facilitates parallel compound synthesis.
描述了使用市售机器人工作站对包含72个成员的2-烷硫基苯并咪唑16和苯并咪唑啉-2-酮17文库进行自动化聚合物辅助溶液相(PASP)合成。通过结合自动化水相后处理、在线清除和“捕获与释放”方案,无需常规色谱纯化即可直接获得所需化合物,产率良好且纯度优异。所描述的合成展示了如何将手动和自动化设备一起使用,以提供一种促进平行化合物合成的通用方法。