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Preparation of 14 C‐ and 18 O‐labeled 2‐[2‐methoxy‐4‐(methylsulfinyl)phenyl]‐1H‐imidazo[4,5‐c]‐pyridine hydrochloride (LY175326), a cardiotonic with inotropic and vasodilator activities
Author(s) -
Kau Don,
Krushinski Joseph H.,
Robertson David W.
Publication year - 1985
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.2580221007
Subject(s) - chemistry , sulfone , hydrochloride , pyridine , benzoic acid , inotrope , medicinal chemistry , chemical synthesis , bicyclic molecule , stereochemistry , organic chemistry , in vitro , biochemistry , endocrinology , medicine
Two different forms of 14 C‐labeled 2‐methoxy‐4‐(methylthio) benzoic acid were prepared and employed in the synthesis of 14 C‐labeled 2‐[2‐methoxy‐4‐(methylsulfinylphenyl]‐lH‐imidazo‐[4,5‐c]pyridine hydrochloride (LY175326), a cardiotonic with inotropic and vasodilator activities that is currently in clinical trials. The synthetic procedures described in this report allowed the introduction of the 14 C‐label in the antepenultimate step. Additionally, an 18 O‐labeled form of LY175326 was synthesized to facilitate kinetic analysis of the formation of its sulfide and sulfone metabolites.