Kiana Shahbazkhani - Medicinal Chemistry Research Laboratory, Shiraz University of Technology, Shiraz, ۷۱۵۵۷-۱۳۸۷۶, Iran
Mohammad Navid Soltani Rad - Medicinal Chemistry Research Laboratory, Shiraz University of Technology, Shiraz, ۷۱۵۵۷-۱۳۸۷۶, Iran

In this paper the design and synthesis of some novel ۸-Caffeinyl-Piperazinyl Triazolyl derivatives as potential and promising bioactive compounds has been described. These compounds were acquired by coupling of synthesized alkyl or aryl azides and already synthesized ۸-bromocaffeine (۸-BC). The preparation of alkyl/aryl azide was performed from NaN۳ with miscellaneous alkyl/aryl halides through the [۳+۲] Hüisgen ۱,۳-dipolar copper-catalyzed azide-alkyne cycloaddition (CuAAC), respectively. The ۸-BC was obtained via bromination of caffeine using NBS. and finally good to excellent of titles compounds were attained through the reaction of ۸-piperazinyl caffeine propargyl and azides in the presence of efficient catalyst in THF.

Caffeine, Hüisgen cycloaddition, Triazole, ۸-BC