Synthesis and Antidepressant Activity of 8-Amino-Substituted 1-Butyl-3-Methylxanthines Containing a Thietane Ring

A series of 8-amino-substituted 1-butyl-3-methylxanthines containing a thietane ring were obtained in 47 – 96% yields by reacting 7-(thietanyl-3)-, 7-(1-oxothietanyl-3)-, and 7-(1,1-dioxothietanyl-3)-8-bromo-1-butyl-3-methylxanthines with piperidine and morpholine. Reaction of 8-amino-substituted 1-butyl-3-methyl-7-(1,1-dioxothietanyl-3)xanthines with sodium ethoxide synthesized 8-amino-substituted 1-butyl-3-methylxanthines in 85 – 98% yields. The structures of the compounds were confirmed by IR and PMR spectroscopy. The synthesized compounds exhibited antidepressant activity.