Synthesis of [ 14 C]‐labelled repinotan hydrochloride and its major metabolite M‐6 | Zendy

Seidel D. | Zendy; Conrad M. | Zendy; Schoof Y. | Zendy; SchoheLoop R. | Zendy

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

Author(s) -

Seidel D.,

Conrad M.,

Schoof Y.,

SchoheLoop R.

Publication year - 2002

Publication title -

journal of labelled compounds and radiopharmaceuticals

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.432

H-Index - 47

eISSN - 1099-1344

pISSN - 0362-4803

DOI - 10.1002/jlcr.629

Subject(s) - chemistry , moiety , acetophenone , hydrochloride , metabolite , phenol , yield (engineering) , stereochemistry , ring (chemistry) , carbon 14 , chemical synthesis , medicinal chemistry , organic chemistry , catalysis , in vitro , biochemistry , materials science , physics , quantum mechanics , metallurgy

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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