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Paper | Regular issue | Vol 53, No. 1, 2000, pp.127-134
Published online, 1st January, 1970
DOI: 10.3987/COM-99-8738
A Facile and Convenient Synthetic Method for Fluorine-containing 1H-Pyrrolo[3,2-h]quinolines

Etsuji Okada* and Norikado Tsukushi

*Department of Chemical Science and Engineering, Faculty of Engineering, Kobe University, Rokkodai-cho, Nada-ku, Kobe 657-8501, Japan


Aromatic nucleophilic nitrogen-nitrogen exchange reaction of N,N dimethyl-5,7-bis(trifluoroacetyl)-8-quinolylamine (1) with some amino acid derivatives gave the corresponding N-[5,7-bis(trifluoroacetyl)-8-quinolyl]amino acid derivatives (2) in excellent yields. Base-catalyzed cyclization of 2 afforded fluorine-containing 1H-pyrrolo[3,2-h]quinolines (3, 4) in high yields.