Preparation of 3-substituted-2-pyridin-2-ylindoles:: regioselectivity of Larock's indole annulation with 2-alkynylpyridines

A regioselective Larock approach to 3-substituted-2-pyridin-2-ylindoles from 2-alkynylpyridines and 2-iodoanilines is described herein. The unexpectedly high regioselectivity can be rationalized by a combination of steric, coordinative and electronic effects. (C) 2007 Elsevier Ltd. All rights reserved.