Towards the Syntheses of N—H and N-Alkylated Derivatives of Meridianins.

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 H-1 and C-13 NMR spectroscopy, NOE experiments and X-ray analysis.