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Synthesis of [1,2‐ 3 H]ethylamine hydrochloride and [ 3 H]‐labeled apadenoson for a human ADME study
Author(s) -
Hong Yang,
Bonacorsi Samuel J.,
Tian Yuan,
Gong Sharon,
Zhang Donglu,
Humphreys W. Griffith,
Balasubramanian Balu,
Cheesman Edward H.,
Zhang Zhiqin,
Castner James F.,
Crane Paul D.
Publication year - 2008
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.1495
Subject(s) - chemistry , ethylamine , hydrochloride , yield (engineering) , tritium , radiochemistry , radiosynthesis , agonist , amine gas treating , chemical synthesis , nuclear chemistry , organic chemistry , receptor , in vitro , in vivo , biochemistry , materials science , physics , nuclear physics , metallurgy , microbiology and biotechnology , biology
Tritium‐labeled [1,2‐ 3 H]ethylamine hydrochloride was prepared through a multiple‐step sequence in high radioactive specificity. The labeled amine was isolated in high purity following cartridge filtration and used subsequently in the synthesis of [ N ‐ethyl‐1,2‐ 3 H]apadenoson, an adenosine A 2a receptor agonist. The overall yield for this transformation was 56% and the radiochemical purity of the final product was greater than 99%. Copyright © 2008 John Wiley & Sons, Ltd.