Synthesis of 14C-labeled E4010

被引:1
作者
Watanabe, N. [1 ]
Tokumura, T. [1 ]
Nakamura, T. [1 ]
机构
[1] Tsukuba Research Laboratories, Eisai Co., Ltd., 5-1-3 Tokodai, Tsukuba, Ibaraki 300-2635, Japan
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D O I
10.1002/jlcr.509
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摘要
14C-Labeled E4010, [4-(3-chloro-4-methoxybenzyl)amino-1-(4-hydroxy) -piperidino]-6-[4-14C]phthalazinecarbonitrile monohydrochloride was synthesized for drug metabolism and pharmacokinetic studies using [1-chloro-4-(3-chloro-4-methoxybenzyl)amino]-6-[4- 14C]phthahizinecarbonitrile as the starting material. The radiochemical yield was 33.4%. The specific radioactivity and radiochemical purity, as determined by radio-HPLC and LSC, were 4.77 MBq/ mg and 99.8%, respectively. Copyright © 2001 John Wiley & Sons, Ltd.
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页码:843 / 847
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