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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
Abstract 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%.