High specific activity tritium labeling of vitamin D derivative RO275646

The octahydroindenone intermediate was tritium labeled using T2O isotope exchange labeling, and then elaborated to the vitamin D derivative RO275646. Though this method of labeling was expected to give the minor isomer, it was the shortest and most convenient route to the high specific activity meta...

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Bibliographic Details
Published in:Journal of labelled compounds & radiopharmaceuticals 2005-12, Vol.48 (14), p.1013-1023
Main Authors: de Keczer, Steve A., Lane, Tim S., Voronin, Tatyana, Masjedizadeh, Mohammad R.
Format: Article
Language:English
Subjects:
Biological and medical sciences
Contrast media. Radiopharmaceuticals
exchange labeling
Medical sciences
minor isomer
Pharmacology. Drug treatments
T2O
tritium
vitamin D
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Summary:The octahydroindenone intermediate was tritium labeled using T2O isotope exchange labeling, and then elaborated to the vitamin D derivative RO275646. Though this method of labeling was expected to give the minor isomer, it was the shortest and most convenient route to the high specific activity metabolically stable labeled sites. A total of 34 mCi (from two separate runs) at 64 Ci/mmol of [3H]‐RO275646 were prepared by this method. Copyright © 2005 John Wiley & Sons, Ltd.
ISSN:0362-4803
1099-1344
DOI:10.1002/jlcr.1014