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Synthesis of the antiinflammatory prodrug RS‐42169‐ 14 C
Author(s) -
Parnes Howard,
Huang Glenn T.
Publication year - 1995
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.2580360106
Subject(s) - chemistry , prodrug , yield (engineering) , cycloaddition , carbonation , sequence (biology) , chemical synthesis , specific activity , combinatorial chemistry , stereochemistry , chromatography , radiochemistry , nuclear chemistry , organic chemistry , in vitro , catalysis , biochemistry , enzyme , metallurgy , materials science
Abstract A facile synthesis of the antiinflammatory agent RS‐42169‐ 14 C, based on a carbonation/cycloaddition sequence is described. The product was obtained in 36% yield from Ba 14 CO 3 at a specific activity of 52 mCi/mmole. The design of the six step sequence was such that pure intermediates were isolated by extractive workup, and only a single chromatographic purification was required.

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