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The synthesis of glycine receptor radioligands [21, 22‐ 3 H] dihydrostrychnine and [2‐ 3 H] strychnine at high specific activity
Author(s) -
Filer Crist N.,
Ahern David G.
Publication year - 1989
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.2580270309
Subject(s) - strychnine , chemistry , yield (engineering) , glycine , catalysis , homogeneous , specific activity , medicinal chemistry , glycine receptor , chemical synthesis , tritium , stereochemistry , organic chemistry , in vitro , biochemistry , amino acid , materials science , physics , metallurgy , thermodynamics , enzyme , nuclear physics
Strychnine ( 1a ) was reduced with tritium gas via heterogeneous catalysis to yield [21, 22‐ 3 H] dihydrostrychnine ( 2b ) at 31 Ci/mmol and via homogeneous catalysis to yield 2b at 50 Ci/mmol. [2‐ 3 H] Strychnine ( 1b ) at 25 Ci/mmol was prepared by the catalytic reductive tritiation of 2‐iodostrychnine ( 4 ). Other polyhalo strychnine analogues were synthesized in an attempt to prepare [ 3 H] strychnine at even higher specific activity.