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Synthesis of [2-14C] fantofarone or 1-[4-[3-N-methyl N-[3,4-dimethyl β-phenethyl] amino propyloxy] benzene sulfonyl]-2-isopropyl [2-14C] indolizine

✍ Scribed by P. Pointeau; Y. Berger


Publisher
John Wiley and Sons
Year
1994
Tongue
French
Weight
303 KB
Volume
34
Category
Article
ISSN
0022-2135

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✦ Synopsis


Abstract

Sodium [1‐^14^C] isobutyrate: 1 was obtained by carbonation of isopropyl magnesium bromide with ^14^CO~2~. From: 1 [1‐^14^C] isobutyryl chloride: 3 was prepared, which through the successive actions of diazomethane and hydrogen bromide gave rise to 1‐bromo 3 methyl [2‐^14^C] 2‐butanone: 5.

The latter lead to the indolizine: 6 which by a route patterned after that used to make unlabelled Fantofarone gave the [2‐^14^C‐indolizyl] Fantofarone: 8 (specific radioactivity: 58.2 mCi/mMole) overall yield 9.9% based on [^14^C] BaCO~3~.


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