✦ LIBER ✦

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

✍ Scribed by Samuel J. Bonacorsi Jr; Richard C. Burrell; George M. Luke; Jeffrey S. DePue; J. Kent Rinehart; Balu Balasubramanian; Lisa J. Christopher; Ramaswamy A. Iyer

Publisher: John Wiley and Sons
Year: 2007
Tongue: French
Weight: 124 KB
Volume: 50
Category: Article
ISSN: 0022-2135
DOI: 10.1002/jlcr.1148

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✦ Synopsis

Abstract

A reliable synthesis of ^14^C 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 ^14^C 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 [^14^C]buspirone. The final product was isolated in reasonable yield with a radiochemical purity of 99.8%. Copyright © 2007 John Wiley & Sons, Ltd.

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