✦ LIBER ✦

Super high specific activity tritium labelled receptor ligands - I. The use of polybromodiphenylacetic acid as a tritiation substrate. Synthesis of a tritium labelled sodium-channel blocker and angiotensin II antagonist with super high specific activity

✍ Scribed by Leyi Gong; Howard Parnes

Publisher: John Wiley and Sons
Year: 1996
Tongue: French
Weight: 406 KB
Volume: 38
Category: Article
ISSN: 0022-2135
DOI: 10.1002/(sici)1099-1344(199601)38:1<31::aid-jlcr806>3.0.co;2-c

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✦ Synopsis

We describe herein the synthesis of polybromodiphenylacetic acid (&), a fragment common to the tritiation substrates (a) and (JJ) of the sodium channel blocker, PD-85639 (1) and the angiotensin II inhibitor EXP-655 (2) respectively. Preparation of (a) and (11) followed by reductive debromonation with carrier free tritium gas furnished the corresponding receptor ligands (1) and (2) having specific activities of 180 Cilmmole and 209 Ci/mmole, respectively.