Synthesis of (±)-depentylperhydrohistrionicotoxin

Abstract
Palladium (0)-catalysed cyclisation of 3-acetoxy-1-(4-aminoalkyl) cyclohexenes provides convenient access to the 1-azaspiro [5.5] undecane ring system found in the histrionicotoxins. Hydroboration of the 7-butyl derivative (4; R1= Bun, R2= H) and oxidation of the purified borane adduct with trimethyl-amine oxide afforded N-benzyldepentylperhydrohistrionicotoxin, which was readily converted into (±)-depentylperhydrohistrionicotoxin by hydrogenolysis over palladium–carbon.

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