Design and Synthesis of Fused Pyridine Building Blocks for Automated Library Generation
作者:Helena Mora‐Radó、Werngard Czechtizky、María Méndez、Joseph P. A. Harrity
DOI:10.1002/cmdc.202000852
日期:2021.1.19
We demonstrate that a diboration‐electrocyclization sequence provides access to a range of pyridine‐fused, small‐molecule boronic ester building blocks, and that these are amenable to high‐throughput synthesis leading to biaryl and ether‐linked compound libraries. Moreover, the implementation of an integrated physicochemical and ADME profiling workflow allows accelerated design of novel lead compounds
我们证明了二硼化-电环化序列可以访问一系列吡啶稠合的小分子硼酸酯结构单元,并且这些结构单元适用于高通量合成,从而产生联芳基和醚连接的化合物库。此外,整合物理化学和 ADME 分析工作流程的实施允许加速设计用于药物发现项目的新型先导化合物。