Published in: Journal, Volume : 45, Issue : 6, Pages : 1275-1277
Author : Blass, Benjamin E.; Srivastava, Anil; Coburn, Keith R.; Faulkner, Amy L.; Janusz, John J.; Ridgeway, James M.; Seibel, William L.
Abstract : The solid-phase synthesis of a series of imidazo[1,2-b]pyrazol-2-ones, an interesting 5,5-fused ring system, based on diverse set of hydrazine acids and malonitriles is described. The method involves formation of 5-aminopyrazoles on solid support and subsequent cyclizative cleavage off the resin. Compounds were obtained in acceptable to excellent yields and are suitable for biol. evaluation without further purification Example compounds thus prepared included 1,8-dihydro-3-[[4-(trifluoromethoxy)phenyl]methyl]-6H-imidazo[1,2-b]thieno[3,4-d]pyrazol-2(3H)-one (I) and 6-(1,1-dimethylethyl)-3-[[4-(trifluoromethoxy)phenyl]methyl]-1H-imidazo[1,2-b]pyrazol-2(3H)-one (II).