Abstract: A process is provided for preparing novel substituted or unsubstituted 4(5)-.omega.-aminoalkyl)imidazoles of the formula ##STR1## wherein n is 1 to 6, R.sub.1 is hydrogen or a linear, branched or cyclic, saturated or unsaturated alkyl group having 1-6 C-atoms or a phenyl ring being unsubstituted, or mono- or di-substituted with groups such as lower alkyl, halogen, alkoxy, methylenedioxy or a combination thereof, and R.sub.2 is hydrogen or methyl. The process comprises brominating an .omega.-phthalimidoalkan-2-one with bromine in anhydrous methanol to a 1- or 3-bromo-.omega.-phthalimido-alkan-2-one, subjecting said derivative to ring closure with an amidine in N.N-dimethylformamide with potassium carbonate under mild conditions followed by hydrolytic separation of the phthalic residue. Pharmaceutical compounds, compositions and a method of treatment are also provided.
Type:
Grant
Filed:
December 3, 1990
Date of Patent:
March 2, 1993
Assignee:
Cedona Pharmaceuticals B.V.
Inventors:
John C. Eriks, Henderikus van der Goot, Hendrik Timmerman, Jan G. Koper