Synthesis of [1,2‐ 3 H]ethylamine hydrochloride and [ 3 H]‐labeled apadenoson for a human ADME study | Zendy

Hong Yang | Zendy; Bonacorsi Samuel J. | Zendy; Tian Yuan | Zendy; Gong Sharon | Zendy; Zhang Donglu | Zendy; Humphreys W. Griffith | Zendy; Balasubramanian Balu | Zendy; Cheesman Edward H. | Zendy; Zhang Zhiqin | Zendy; Castner James F. | Zendy; Crane Paul D. | Zendy

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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.

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