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Synthesis of 3 H‐ and 14 C‐labeled tracers for studies of functional monoamine oxidase activity
Author(s) -
Halldin Christer,
Bjurling Peter,
Långström Bengt,
Macgregor Robert R.,
Fowler Joanna S.,
Wolf Alfred P.
Publication year - 1988
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.2580250508
Subject(s) - chemistry , clorgyline , methyl iodide , alkylation , iodide , carbon 14 , amine gas treating , monoamine oxidase , formaldehyde , yield (engineering) , specific activity , radiochemistry , medicinal chemistry , organic chemistry , catalysis , enzyme , physics , materials science , quantum mechanics , metallurgy
The 3 H‐labeling of clorgyline, L‐deprenyl, N,N‐dimethylphenethyl amine and N‐methylphenethyl amine as well as the 14 C‐labeling of clorgyline and L‐deprenyl are described. Labeling was accomplished by N‐alkylation of the free base of the corresponding desmethyl compound, using 3 H‐methyl iodide, or by a reductive alkylation using 14 C‐formaldehyde. The crude products were purified by semipreparative HPLC. The total radiochemical yield was 31‐65% based on 3 H‐methyl iodide and 60% based on 14 C‐formaldehyde. The radiochemical purity was greater than 99%.