Transient directing groups (TDGs) have been demonstrated to promote the in situ generation and elimination of directing groups, thereby providing an efficient strategy for C–H functionalization. This study utilizes the in situ formation of imines between amino acids and aromatic aldehydes. Under copper‐mediated conditions, an ortho ‐C–H etherification reaction between aromatic aldehydes and phenols/alcohols was achieved. To the best of our knowledge, this represents the first example of a TDG‐mediated reaction involving phenol substrates. The utility of this strategy has been demonstrated through multiple applications, including the late‐stage diversification of drug analogs.
Ma et al. (Thu,) studied this question.