Pd-catalyzed direct C2-acylation and C2,C7-diacylation of indoles: pyrimidine as an easily removable C-H directing group

Pyrimidine is successfully used as an easily removable C(sp(2))-H directing group for the synthesis of 2-acyl indoles and 2,7-diacyl indoles through direct C-H functionalization using a Pd-catalyst from 1-(pyrimidin-2-yl)-1H-indoles and aldehydes. Easy removal of the pyrimidine directing group using EtONa in DMSO provides C2-acyl indoles.