H. V. Secor, R. Izac, S. Hassam
May 1, 1994
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Journal
Journal of Labelled Compounds and Radiopharmaceuticals
Abstract
[Methyl-14C]-N-methylputrescine was prepared from [14C]methylamine hydrochloride in five steps. Reaction of benzaldehyde and [14C]methylamine (10 mCi) followed by catalytic hydrogenation yielded [methyl-14C]-N-methylbenzylamine. The key step in this process is the alkylation of [methyl-14C]-N-methylbenzylamine in aqueous medium with 4-bromobutyronitrile. The radiochemical purity of the final product after two successive catalytic hydrogenations was in excess of 97%. The radiochemical yields in two successive runs were 26 and 38%, based on starting [14C]methylamine, with specific activities of 22 and 23 mCi/mmol, respectively. This sequence provides a convenient and efficient regioselective radiosynthesis of [methyl-14C]-N-methylputrescine.