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Tritiation of CEP-1347 at high specific activity using several methods

โœ Scribed by Judith A. Egan; Crist N. Filer; Scot Pounds; Thomas Connors; Ernest Knight Jr; Robert L. Hudkins


Publisher
John Wiley and Sons
Year
2005
Tongue
French
Weight
88 KB
Volume
48
Category
Article
ISSN
0022-2135

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โœฆ Synopsis


Thiomethylenes-3 H] CEP-1347 (5) was synthesized by the tritiation of diformyl precursor 3 with NaB 3 H 4 followed by treatment with ethanethiol. [Methyl ester-3 H] CEP-1347 ( 7) was prepared at even higher specific activity by the alkylation of precursor 6 with C 3 H 3 I.


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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 wit