An efficient and simple aminobenzannulation reaction: pyrrolidine as a trigger for the synthesis of 1-amino-acridines.

[reaction: see text] A new aminobenzannulation methodology has been developed and applied successfully to the synthesis of 1-amino-acridines. The key and last step goes through an enamine intermediate that was detected in some cases. When pyrrolidine and powdered 4 A molecular sieves were used, the enamine synthesis and the aminobenzannulation step took place subsequently, whereas for other secondary amines, neutral Al(2)O(3) or PtCl(2) catalysis was necessary.