Affiliation:
1. Department of Biotherapy Cancer Center and State Key Laboratory of Biotherapy West China Hospital Sichuan University Chengdu Sichuan 610041 People's Republic of China
2. Antibiotics Research and Re-evaluation Key Laboratory of Sichuan Province Sichuan Industrial Institute of Antibiotics School of Pharmacy Chengdu University Chengdu 610106 People's Republic of China
Abstract
AbstractA ruthenium‐catalyzed C(sp2)−H acyloxylation of 2‐aroyl pyridine derivatives with simple sodium carboxylate utilizing transformable directing groups is described. This protocol features broad functional group tolerance and chemo‐ and regio‐selectivity, providing the acyloxylation products in 45%‐84%yield. Furthermore, the synthetic utility of this protocol was demonstrated by the late‐stage functionalization of pharmaceutical compounds. Notably, the acyloxylation products could be further transformed into a variety of useful heterocycles under mild conditions.
Funder
Natural Science Foundation of Sichuan Province