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Synthesis of (+)‐N‐(6‐Ethoxy[2,4‐ 3 H]phenyl)‐N‐(1,2,2‐trimethylpropyl)‐2‐nitroethene‐1,1‐diamine ([ 3 H]BAY x 9228)
Author(s) -
Pleiß U.,
Lenfers J.B.,
Schmitt P.
Publication year - 1993
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.2580330802
Subject(s) - chemistry , diamine , alkoxy group , enantiomer , hydroxide , halogenation , catalysis , high performance liquid chromatography , chemical synthesis , medicinal chemistry , organic chemistry , alkyl , biochemistry , in vitro
The synthesis of tritium‐labelled (+)‐N‐(6‐Ethoxy[2,4‐ 3 H]phenyl)‐N‐(1,2,2‐trimethylpropyl)‐2‐nitroethene‐1, 1‐diamine ([ 3 H]BAY x 9228) a pottassium channel opener, was achieved by dehalogenation of a dibrominated racemic precursor using palladium hydroxide on charcoal as catalyst. The separation into the enantiomers was achieved by an chiral HPLC‐column. The specific activity was 47.9 Ci/mmol (1.8 TBq/mmol).