Synthesis of azole-containing allylamines

Reactions of benzimidazole-2-thiol with N-alkyl-1-aza-1,3-enynes

“…Recently, considerable attention has been focused on the heterocyclization reactions of 1-aza-1,3-enynes resulting from addition of various nucleophilic reagents [3]. Benzimidazole-2-thiol derivatives readily participate in the substitution and addition (at activated double or triple bond) reactions resulting in formation of heterocyclic or acyclic products [7,8]. Benzimidazole-2-thiol and its derivatives are known for anxiolytic activity [9]; some of them inhibit chymases (enzymes responsible for activation of interleukin-1β, serving among the major mediators of non-specific inflamematory forms of protection) [10].…”