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 | Zendy

Kau Don | Zendy; Krushinski Joseph H. | Zendy; Robertson David W. | Zendy

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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.

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