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Synthesis of the serotonin ligands, RS-56532-14C and RS-66331-14C from a common labelled intermediate

✍ Scribed by Mohammad R. Masjedizadeh; Howard Parnes

Publisher
John Wiley and Sons
Year
1993
Tongue
French
Weight
509 KB
Volume
33
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

Two approaches towards the synthesis of 3‐chloro‐4‐amino‐1,8‐naphthalic anhydride‐[^14^C], which served as the common intermediate in the preparation of the two title compounds, are described. Although nucleophilic incorporation of the label via KCN was superior to an electrophilic sequence using CO~2~, the latter approach was adopted since the nitrile could not be hydrolyzed to the desired acid. The specific activities of RS‐56532‐^14^C and RS‐66331‐^14^C were 56.8 mCi/mmol and 53.7 mCi/mmol, respectively.

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