Synthesis of the anxiolytic agent [14C] 6-hydroxy-buspirone for use in a human ADME study

A reliable synthesis of 14C labeled 6‐hydroxy‐buspirone is described. The molecule belongs to a unique class of compounds with the potential for anxiolytic activity. A radiolabeled analog was prepared to support the development of 6‐hydroxy‐buspirone. Specifically, a labeled variant was designed to...

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Bibliographic Details
Published in:Journal of labelled compounds & radiopharmaceuticals 2007-02, Vol.50 (2), p.65-71
Main Authors: Bonacorsi Jr, Samuel J., Burrell, Richard C., Luke, George M., DePue, Jeffrey S., Kent Rinehart, J., Balasubramanian, Balu, Christopher, Lisa J., Iyer, Ramaswamy A.
Format: Article
Language:English
Subjects:
6-hydroxy-buspirone
Biological and medical sciences
buspirone
carbon-14 synthesis
Contrast media. Radiopharmaceuticals
Medical sciences
Neuropharmacology
Pharmacology. Drug treatments
Psycholeptics: tranquillizer, neuroleptic
Psychology. Psychoanalysis. Psychiatry
Psychopharmacology
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Summary:A reliable synthesis of 14C labeled 6‐hydroxy‐buspirone is described. The molecule belongs to a unique class of compounds with the potential for anxiolytic activity. A radiolabeled analog was prepared to support the development of 6‐hydroxy‐buspirone. Specifically, a labeled variant was designed to meet the requirements of a human adsorption‐distribution‐metabolism‐elimination (ADME) study. Multiple 14C labels were needed to fully track the potential metabolic transformation of the molecule. Labeled 6‐hydroxy‐buspirone was prepared by oxidation of separately labeled versions of [14C]buspirone. The final product was isolated in reasonable yield with a radiochemical purity of 99.8%. Copyright © 2007 John Wiley & Sons, Ltd. A synthesis of 14C labeled 6‐hydroxy‐buspirone is described. The molecule was labeled in multiple positions to support a human ADME study. The product was isolated with a radiochemical purity of 99.8%. Copyright © 2007 John Wiley & Sons, Ltd.
ISSN:0362-4803
1099-1344
DOI:10.1002/jlcr.1148