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Synthesis of 14C-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 (14C-E6123)

✍ Scribed by Shuhei Miyazawa; Kazuo Okano; Kazutomi Kusano; Kyoichi Tadano; Shigeru Tanaka; Teruaki Yuzuriha; Yoshimasa Machida; Lsao Yamatsu

Publisher
John Wiley and Sons
Year
1991
Tongue
French
Weight
197 KB
Volume
29
Category
Article
ISSN
0022-2135

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✦ Synopsis

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%.

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