European Journal of Organic Chemistry, Год журнала: 2024, Номер 27(24)
Опубликована: Апрель 22, 2024
Abstract The electrophilic activation of 2 H ‐azirines with triflic anhydride (Tf O) for an addition/cyclization reaction producing 2‐aryl‐pyrido[2,3‐ b ]pyrazines regioselectively is described. This proceeds via nucleophilic addition 3‐amino‐2‐fluoropyridines onto 1‐trifloyl‐aziridin‐2‐yl triflates and subsequent cyclization S N Ar. Desulfonylation oxidation provides a single regioisomer the aza‐bicyclic heterocycle after treatment Et 3 N. Optimization conditions lead to range in isolated yields 20 % 60 %.
Язык: Английский