68020-39-3Relevant academic research and scientific papers
Synthesis of five- and six-membered cyclic guanidines by guanylation with isothiouronium iodides and amines under mild conditions
Aoyagi, Naoto,Endo, Takeshi
, p. 442 - 448 (2017/02/24)
Cyclic guanidine hydroiodides were obtained in one step by the reactions of isothiouronium iodides with an equimolar amount of various amines in tetrahydrofuran. The obtained hydroiodides were neutralized with sodium hydroxide or anionic exchange resin to afford the corresponding substituted cyclic guanidines in quantitative yields.
Substituted 6,7-dihydroimidazo[1,2-al]purin-9 (4H)-ones
Temple Jr.,Yevich,Catt,Owens,Hanning,Covington,Seidehamel,Dungan
, p. 1188 - 1198 (2007/10/02)
The synthesis of a series of substituted 6,7-dihydroimidazo[1,2-a]purin-9(4H)-ones is described. Several members of the series exhibit enhanced antiallergic and bronchodilator activity and reduced side effects as compared to theophylline. Structure-activity relationships and metabolic considerations are discussed for the series. Analogues substituted with a 4-(4-chlorobenzyl) moiety, such as 33 and 40, show an optimal balance of antiallergic and bronchodilator activity and are of particular interest. Compound 33 is significantly more potent than theophylline against both metacholine- and antigen-induced bronchospasms, does not affect spontaneous motor activity, and shows minimal cardiovascular effects in the rat.
