2007 年 55 巻 7 号 p. 1039-1043
We synthesized the six presumed metabolites (2—7) of 4-(2-methyl-1H-imidazol-1-yl)-2,2-diphenylbutanamide [KRP-197/ONO-8025, 1], a urinary incontinence therapeutic agent, in order to confirm the structures of the metabolites. Metabolite (2) was synthesized via glucuronidaion of compound (1) and methyl 2,3,4-tri-O-benzoyl-1-methanesulfonyl-α-D-glucopyranuronate. Metabolite (3) was synthesized via 3-(tert-butoxycarbonyl)-2-methyl-1,3-imidazolidine-4,5-dione. Metabolites (4—7) were synthesized via 4-amino-2-diphenylbutanamide, respectively. The structures of the metabolites (2—7) in humans were identified by means of synthesis of the authentic compounds.
