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Synthesis of tritium- and deuterium-labeled budesonide

✍ Scribed by Bachir Latli; Dhileep Krishnamurthy; Chris Senanayake

Publisher
John Wiley and Sons
Year
2008
Tongue
French
Weight
178 KB
Volume
51
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

Tritium‐labeled budesonide was prepared by the selective reduction of a double bond in the butenylenedioxy side chain using carrier‐free tritium and palladium on carbon as a catalyst in absolute ethanol. Although the reduction gave a mixture of the desired product and the expected byproducts resulting from over reduction of the other double bonds in ring A, the desired tritium‐labeled budesonide was easily isolated by reverse phase HPLC and with specific activity of 54 Ci/mmol. [D~8~]‐budesonide was prepared from 16α‐hydroxyprednisolone and D~8~‐butyraldehyde in 1,4‐dioxane in the presence of perchloric acid. The isotopic enrichment was found to be more than 99 atom% D. Copyright © 2008 John Wiley & Sons, Ltd.

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