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

• DOI: 10.1007/s11094-020-02114-0
• Publication Date: 2020-02-25T16:02:42Z
• Authors: Yu. V. Shabalina; F. A. Khaliullin; I. L. Nikitina; A. F. Miftakhova; R. M. Sharafutdinov
• Keywords: 0301 basic medicine; 0303 health sciences; 03 medical and health sciences; 3. Good health

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.