| abstract |
A process for preparing polyazamacrocyclic compounds using a nucleophilic imidazoline with (A) an ethylene oxide or an ethylene carbonate, in an aprotic solvent, followed by intramolecular amination, and then either basic or acidic hydrolysis; or (B) an electrophilic substrate, in a polar solvent, optionally in the presence of a non-nucleophilic base, to form an intermediate, followed by basic hydrolysis; or (C) an electrophilic substrate, in a polar solvent, optionally in the presence of a non-nucleophilic base, followed by prolonged heating in a polar solvent or by treatment with a peroxide solution, followed by basic hydrolysis to form a urea, then basic hydrolysis under pressure; and separating the desired polyazamacrocycle. The compounds so prepared are useful in pharmaceutical applications. |