Thombal Raju S, Lee Yong Rok
School of Chemical Engineering, Yeungnam University, Gyeongsan 38541, Republic of Korea.
Org Lett. 2020 May 1;22(9):3397-3401. doi: 10.1021/acs.orglett.0c00877. Epub 2020 Apr 8.
A Pd(II)-catalyzed C(sp)-H/C(sp)-H coupling/annulation of anilides and α-dicarbonyl compounds for the synthesis of diverse -acyl indoles is described. The reaction is achieved by cascade C-H activation, coupling, and intramolecular cyclization. This protocol provides a variety of indoles with high functional group tolerance and excellent regioselectivity. The utility of this protocol is demonstrated by transforming the synthesized compound into diversely functionalized analogues.
描述了一种用于合成多种β-酰基吲哚的钯（II）催化的苯胺和α-二羰基化合物的C（sp）-H/C（sp）-H偶联/环化反应。该反应通过级联C-H活化、偶联和分子内环化来实现。该方法提供了多种具有高官能团耐受性和优异区域选择性的吲哚。通过将合成的化合物转化为多种功能化类似物，证明了该方法的实用性。
