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A labelled hypocholesteremic agent, preparation OF 2‐(2‐pyridine)‐1‐(3‐chlorophenyl)‐2‐phenyl‐1‐methylethanol uniformly tritiated on the 2‐phenyl ring
Author(s) -
Hansen D. W.,
Van Eeckhout E. Den,
Drach J. C.,
Burckhalter J. H.,
Sinsheiraer J. K.
Publication year - 1974
Publication title -
journal of labelled compounds
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0022-2135
DOI - 10.1002/jlcr.2590100205
Subject(s) - pyridine , tritium , benzene , ring (chemistry) , chemistry , enantiomer , specific activity , nuclear chemistry , radiochemistry , medicinal chemistry , stereochemistry , organic chemistry , physics , nuclear physics , enzyme
2‐(2‐Pyridine)‐1‐(3‐chlorophenyl)‐2‐phenyl‐1‐methylethanol (I), containing tritium uniformly distributed in the 2‐phenyl ring, was synthesized in two steps with tritiated benzene as the labelled starting material. An improved procedure was employed for the coupling of m‐chloroacetophenone and 2‐benzylpyridine. The higher melting of two enantiomeric pairs, known for its hypocholesteremic activity in rats, was isolated and found to have a chemical purity of >95% and a specific activity of 0.11 mCi/mmole.