Synthesis of  14 C‐labelled (S)‐(+)‐6‐(2‐chlorophenyl)‐3‐cyclopropanecarbonyl‐8,11‐ dimethyl‐2,3,4,5‐tetrahydro‐8H‐pyrido[4′,3′:4,5]thieno[3,2‐f][1,2,4]triazolo[4,3‐a][1,4]diazepine ( 14 C‐E6123) | Zendy

Miyazawa Shuhei | Zendy; Okano Kazuo | Zendy; Kusano Kazutomi | Zendy; Tadano Kyoichi | Zendy; Tanaka Shigeru | Zendy; Yuzuriha Teruaki | Zendy; Machida Yoshimasa | Zendy; Yamatsu Lsao | Zendy

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Synthesis of 14 C‐labelled (S)‐(+)‐6‐(2‐chlorophenyl)‐3‐cyclopropanecarbonyl‐8,11‐ dimethyl‐2,3,4,5‐tetrahydro‐8H‐pyrido[4′,3′:4,5]thieno[3,2‐f][1,2,4]triazolo[4,3‐a][1,4]diazepine ( 14 C‐E6123)

Author(s) -

Miyazawa Shuhei,

Okano Kazuo,

Kusano Kazutomi,

Tadano Kyoichi,

Tanaka Shigeru,

Yuzuriha Teruaki,

Machida Yoshimasa,

Yamatsu Lsao

Publication year - 1991

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.2580290913

Subject(s) - chemistry , yield (engineering) , hydrazine (antidepressant) , diazepine , chemical synthesis , stereochemistry , bicyclic molecule , medicinal chemistry , ring (chemistry) , organic chemistry , chromatography , in vitro , materials science , metallurgy , biochemistry

14 C‐Labelled (S)‐(+)‐6‐(2‐chlorophenyl)‐3‐cyclopropanecarbonyl‐8,11‐dimethyl‐2,3,4,5‐ tetrahydro‐8H‐pyrido[4′,3′:4,5]thieno[3,2‐f][1,2,4]triazolo[4,3‐a][1,4] diazepine ( 14 C‐E6123), a platelet activating factor receptor antagonist for studying the pharmacokinetic profile of E6123, was synthesized in three steps using [1‐ 14 C] acetyl hydrazine fumarate as the labelled starting material. The final product has high chemical and radiochemical purity with a specific activity of 53.2mCi per mmol (1.97GBq per mmol). The overall radiochemical yield is 6.0%.

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