Regio- and Chemoselective C—H Chlorination/Bromination of Electron-Deficient Arenes by Weak Coordination and Study of Relative Directing-Group Abilities

摘要

Aromatic chlorides are an important class of compounds utilized in drug and natural product syntheses. Today, about 85% of all pharmaceuticals contain or are manufactured using chlorine. By far the most prevalent strategies for preparing aromatic chlorides are still the classic directed ortho lithiation, eletrophilic aromatic substitution, and Sand-meyer reaction. However, these methods usually suffer from one or more limitations including poor regioselectivity, low yield, harsh reaction conditions, long reaction time, and tedious reaction procedures. Therefore, the development of a general, mild, and practical approach to aromatic chlorides is still highly desired because of their significance.