摘要/Abstract

通过实例介绍分析药效基团和C—H活化导向基团的功能作用以及功能转换在药物研发中的应用，归纳总结出许多药效基团，如含氮芳香化合物、氰基、羧基、磺酰胺基等，是理想的C—H活化导向基团，在药物合成的后续阶段引入C—H活化官能团将大大简化并有效提高发现新药的可能性.评述了这个新思维及C—H活化合成方法的最新突破以及其在新药研究中的应用，最后列举了药效基团作为C—H活化导向基团进行药物合成的工业化实例，相信这一新发展将推动药物发明与创新，使药物合成与工艺更趋环境友好.
关键词: 药效基团, 导向基团, C—H活化和官能团化, 功能转换
The functional switch of a C—H activation directing group to a pharmacophore is introduced and analyzed, and the value of the pharmacophore and the application of C—H activation are exemplified. It is concluded that many pharmacophores, such as N-containing heteroaromatic, nitrile, carboxylic acid, amide and sulfonamide groups, are ideal directing groups for C—H activation enabling the subsequent stages of drug synthesis, and showing that there is a correlation between a directing group and a pharmacophore. The late-stage functionalization will greatly simplify and effectively improve the possibility of discovering new drugs and potentially shortening the overall synthesis. The latest breakthroughs of C—H activation and application in the drug discovery process are reviewed as case studies, providing several industrial examples of using a pharmacophore as directing group for drug synthesis. It is believed that this development will promote a more rapid and green drug synthesis.
Key words: pharmacophore, directing group, C—H activation and functionalization, functional switch between pharmacophore and directing group


PDF全文下载地址:

点我下载PDF