Towards the syntheses of <i>N</i>‐H and <i>N</i>‐alkylated derivatives of meridianins

Abstract

Abstract magnified image Novel N ‐H and N ‐alkylated derivatives of meridianins have been synthesized as potential antitumor agents by a two‐step conversion of N ‐tosyl‐3‐acetylindoles or N ‐alkyl‐3‐acetylindoles to the corresponding enaminones using DMF‐DMA, with or without added pyrrolidine. Further cyclization with guanidine gave the corresponding 2‐aminopyrimidines. The structures of the compounds, thus obtained, were proved by 1 H and 13 C NMR spectroscopy, NOE experiments and X‐ray analysis.