Synthesis of [~3H], [~13Cl~5N] and [~14C]Sch 66336 (Sarasar~TM)

摘要

[~3H]Sch 66336 was prepared at a specific activity of 1.35Ci/mmol by Ru(Ph_3P)_3C_2 catalysed exchange with tritiated water. [~13C_2~5N]Sch 66336 was synthesized from potassium [~13C]cyanide and [13C15N2]urea in 29% overall yield from potassium [~13C]cyanide. [~14C]Sch 66336 was synthesized from potassium [~14C]cyanide in 31% yield. A second synthesis, from 7V-Boc-4-hydroxy[~I4C]piperidine, gave [~14C]Sch 66336 labelled in a different site in 19% overall yield.