Aromaticity-Dependent Regioselectivity in Pd(II)-Catalyzed C-H Direct Arylation of Aryl Ureas

Org Lett. 2015 Dec 4;17(23):5918-21. doi: 10.1021/acs.orglett.5b03153. Epub 2015 Nov 17.

Abstract

Palladium-catalyzed C-H direct arylation generally occurs on the ortho-position of directing groups. By comparing meta-arylated products of 2-naphthyl urea to ortho-arylated products of phenyl urea, the ortho- and meta-regioselectivity of aryl ureas were found to depend on the aromaticity of the corresponding aryl substituents. Thus, aromaticity is a new factor which can affect the regioselectivity in C-H direct arylation. The finding was further confirmed by regioselective direct arylation of indole and pyrrole derivatives.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Catalysis
  • Combinatorial Chemistry Techniques
  • Indoles / chemistry*
  • Molecular Structure
  • Naphthalenes / chemistry*
  • Palladium / chemistry*
  • Pyrroles / chemistry*
  • Stereoisomerism
  • Urea / analogs & derivatives*
  • Urea / chemistry*

Substances

  • Indoles
  • Naphthalenes
  • Pyrroles
  • Palladium
  • Urea