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Synthesis of carbon-14 and deuterium labeled 3-isobutyryl-2-isopro-pylpyrazolo [1, 5-a]pyridine

✍ Scribed by Yoshio Nagatsu; Koichi Takagi

Publisher
John Wiley and Sons
Year
1985
Tongue
French
Weight
305 KB
Volume
22
Category
Article
ISSN
0022-2135

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✦ Synopsis

In order to study the metabolic fate of 3-isobutyryl-2-isopropylpyrazolo~1,5-aJpyridine [I, in experimental animals and humans, the synthesis of I labeled with carbon-14 or deuterium was investiqated. Carbon-14 labeled I was obtained from 5 mCi of isobutyric acid-l-14C sodium salt with a 6 7 . 7 % yield. Its specific activity was 2 4 . 7 pCi/mg. with a 1 7 . 0 % yield, which resulted in about 50% replacement of deuterium with hydrogen at the position 7 in I. The release of deuterium apparently did not occur on GC-MS.

The mixture of deuterium labeled I and unlabeled I (2:l mole ratio) supplied nearly the same intensity of triplet ions (ion clusters) used for identification of I and its metabolites.

Deuterium labeled I was synthesized from pyridine-d5

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