Efficient access to azaindoles and indoles |
| |
Authors: | McLaughlin Mark Palucki Michael Davies Ian W |
| |
Institution: | Department of Process Research, Merck Research Laboratories, P.O. Box 2000, Rahway, New Jersey 07065, USA. mark_mclaughlin@merck.com |
| |
Abstract: | Structure: see text] An expedient, catalytic method for the synthesis of diverse azaindoles and indoles, starting from readily available and inexpensive starting materials, is described. Conditions were developed for effective reductive alkylation of electron-deficient o-chloroarylamines, substrates previously viewed as poor partners in this reaction. The derived N-alkylated o-chloroarylamines were elaborated to N-alkylazaindoles and N-alkylindoles via a novel one-pot process comprising copper-free Sonogashira alkynylation and a base-mediated indolization reaction. |
| |
Keywords: | |
本文献已被 PubMed 等数据库收录! |
|