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Synthesis of [14C]-labelled repinotan hydrochloride and its major metabolite M-6

✍ Scribed by D. Seidel; M. Conrad; Y. Schoof; R. Schohe-Loop

Publisher
John Wiley and Sons
Year
2002
Tongue
French
Weight
150 KB
Volume
45
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

For studies of pharmacokinetics and drug metabolism of the new 5‐HT~1A~ agonist repinotan, the ^14^C‐labelled version was synthesized. Starting from [U‐^14^C]phenol, a 10‐step synthesis led to 457 mg (1.58 GBq) of [U‐^14^C]repinotan hydrochloride, labelled uniformly in the aromatic ring of the chromane moiety. For a study in man, a mono‐carbon‐14 labelled substance was required. Therefore a 7‐step synthesis was performed starting from [carbonyl‐^14^C]2‐hydroxy‐acetophenone. The yield was 106 mg (0.396 GBq) of [4‐chromane‐^14^C]repinotan hydrochloride. The carbon‐14 labelled major metabolite, hydroxylated in the 6‐position of the chromane moiety, was synthesised as reference compound. Copyright © 2002 John Wiley & Sons, Ltd.

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