Bicyclic Isosteres of Pyridine/Piperidine: From Synthesis to Applications
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2-Azabicyclo[2.2.2]octanes have been designed, synthesized, and validated biologically as isosteres of piperidine/pyridine. The key reaction step was the cyclization of cyclic alkenyl amines with the KOtBu/I2/CO2 combination. The method proved to be scalable (... ...