Preparation of 14C- and 18O-labeled 2-[2-methoxy-4-(methylsulfinyl)phenyl]-1H-imidazo[4,5-c]-pyridine hydrochloride (LY175326), a cardiotonic with inotropic and vasodilator activities

Two different forms of 14C‐labeled 2‐methoxy‐4‐(methylthio) benzoic acid were prepared and employed in the synthesis of 14C‐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...

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Veröffentlicht in:Journal of labelled compounds & radiopharmaceuticals 1985-10, Vol.22 (10), p.1045-1060
Hauptverfasser: Kau, Don, Krushinski, Joseph H., Robertson, David W.
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container_title Journal of labelled compounds & radiopharmaceuticals
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creator Kau, Don
Krushinski, Joseph H.
Robertson, David W.
description Two different forms of 14C‐labeled 2‐methoxy‐4‐(methylthio) benzoic acid were prepared and employed in the synthesis of 14C‐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 14C‐label in the antepenultimate step. Additionally, an 18O‐labeled form of LY175326 was synthesized to facilitate kinetic analysis of the formation of its sulfide and sulfone metabolites.
doi_str_mv 10.1002/jlcr.2580221007
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subjects Carbon-14
cardiotonic
LY175326
Oxygen-18
positive inotrope
title Preparation of 14C- and 18O-labeled 2-[2-methoxy-4-(methylsulfinyl)phenyl]-1H-imidazo[4,5-c]-pyridine hydrochloride (LY175326), a cardiotonic with inotropic and vasodilator activities
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