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

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

Publisher
John Wiley and Sons
Year
2008
Tongue
French
Weight
189 KB
Volume
51
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

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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