Metal-free selective mono-halodecarboxylation of heteroarenes under mild conditions

R Soc Open Sci. 2018 Jun 20;5(6):180333. doi: 10.1098/rsos.180333. eCollection 2018 Jun.

Abstract

The halodecarboxylation of heteroarene carboxylic acids by treatment with N-bromosuccinimide or N-chlorosuccinimide was performed. This procedure provides a convenient route to synthetically useful mono-halogenated heteroarene intermediates such as halo-indoles, -aza-indoles, -indazoles and -aza-indazoles. The mild conditions employed and simple protocol provides an advantage over traditional halodecarboxylation procedures that require expensive and toxic metal catalysts, basic conditions, time-consuming intermediate isolation and elevated reaction temperatures.

Keywords: halodecarboxylation; mild conditions; selective halogenation.

Associated data

  • figshare/10.6084/m9.figshare.c.4116533