Utility of Japp-Klingemann reaction for the preparation of 5-carboxy-6-chloroindole via Fischer indole protocol

摘要

5-Carboxy-6-chloroindole,a precursor for p38 kinase inhibitor,was prepared from 4-amino-2-chloro-3-iodobenzoicacid by following the Japp-Klingemann synthetic approach.The structures of the key intermediates were also confirmed by X-ray analyses.Computational analysis was helpful in understanding the importance of the substituents at the cyclization step of the synthesis.