Abstract
In an effort to obtain active analgesic and anti-inflammatory agents, alkylation of cycloheptimidazolone and cyclohepta[b]pyrrolone was carried out. Benzylation of 4-and 6-hydroxycycloheptimidazol-2(1H)-one afforded 1-benzyl and 1, 3-dibenzyl derivatives. Benzylation of cyclohepta[b]pyrrol-2(1H)-one afforded 1-and 3-benzyl derivatives. Benzylation of cyclohepta[b]pyrrole-2, 8(1H, 3H)-dione which is considered to be present in many tautomers afforded 3-benzyl, 3, 3-and 1, 3-dibenzyl, 1, 3, 3-tribenzyl and 1, 3-dibenzyl-8-benzyloxy derivatives. By the alkylation of cycloheptimidazol-2(1H)-one and 3-substituted cyclohepta[b]pyrrol-8(1H)-one, a number of 1-alkyl derivatives were prepared. Among these products, 1-benzylcycloheptimidazol-2(1H)-one has been found to be the most active analgesic and anti-inflammatory agent.
