1. Laboratoire de Chimie Hétéro‐Organique, U.F.R. Sciences et Techniques, 6 Av. V. Le Gorgeu — CS 93837 ‐ 29238 Brest Cedex 3, France. Tel.: (33) 2 98 01 61 60;2. fax.: (33) 2 98 01 67 04;3. Services RMN‐RPE, RX, U.F.R. Sciences et Techniques, 6 Av. V. Le Gorgeu — CS 93837 ‐ 29238 Brest Cedex 3, France;4. CNRS, Cell Cycle Group, Station Biologique, BP74, 29682 Roscoff Cedex, France
Abstract:
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 1H and 13C NMR spectroscopy, NOE experiments and X‐ray analysis.
