The synthesis and ring opening of N‐substituted‐2‐oxo‐6‐azaspiro[2,5] octanes

Abstract

N‐Substituted‐4‐piperidones have been reacted with trimethyl sulfoxonium iodide to give the title compounds. These undergo ring opening with lithium aluminum hydride‐aluminum chloride to give piperidine‐4‐methanols which were converted to the chloromethylpiperidines.

N-Benzylpiperidine Derivatives as α7 Nicotinic Receptor Antagonists

“…For this purpose, we explored the activity of less bulky N -benzylpiperidine derivatives, such as chlorides 42 and 43 , alcohols 44 and 45 , and amines 46 , 47 , 48 , 49 , and 50 (Figure ) on α7 nAChRs. The effect of 1 and 10 μM N -benzylpiperidines on the magnitude of α7 nAChR peak currents elicited by ACh is shown in Figure .…”