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Base‐catalyzed deuterium and tritium labelling of 1‐biphenyl‐4‐ylpropane‐1,2‐dione and deuteration of aryl methyl ketones
Author(s) -
Berthelette Carl,
Scheigetz John
Publication year - 2004
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.879
Subject(s) - chemistry , tritium , deuterium , aryl , labelling , catalysis , biphenyl , base (topology) , methyl group , medicinal chemistry , radiochemistry , organic chemistry , group (periodic table) , nuclear physics , mathematical analysis , biochemistry , alkyl , physics , mathematics
A synthesis and a base‐catalyzed exchange reaction was developed under mild conditions to deuterate and subsequently tritiate the methyl group of the base sensitive diketone 1‐biphenyl‐4‐ylpropane‐l,2‐dione depicted in Figure 1. Using Et 3 N as base, deuterium incorporation of the methyl group was 88.9% and the tritium incorporation gave a specific radioactivity of 119 mCi/mmol. The scope of the exchanges was extended to methyl aryl ketones 2–4 . Copyright © 2004 John Wiley & Sons, Ltd.