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[14C] and [3H]-labelling of Ragaglitazar: A dual acting PPARα and PPARγ agonist with hypolipidemic and anti-diabetic activity

✍ Scribed by Jesper B. Kristensen; Steen K. Johansen; Jacob S. Valsborg; Lars Martiny; Christian Foged

Publisher
John Wiley and Sons
Year
2003
Tongue
French
Weight
138 KB
Volume
46
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

Currently, Ragaglitazar is being developed as a drug for the treatment of hyperglycaemia and hyperlipidemia in patients with type 2 diabetes. Here, we report the labelling of Ragaglitazar with carbon‐14 and tritium for in vivo and in vitro investigations. Two different carbon‐14 labelled as well as two different tritium labelled tracers of Ragaglitazar were synthesised. The carbon‐14 label was introduced from either ethyl bromo[2‐^14^C]acetate (5 steps/33% overall yield) or [U‐^14^C]phenoxazine (4 steps/48% overall yield). Tritium was incorporated either by catalytic tritiation of an alkene precursor followed by chiral HPLC separation (2 steps/17% overall yield) or by catalytic tritium–halogen exchange of an aryl bromide precursor (2 steps/68% overall yield). Copyright © 2003 John Wiley & Sons, Ltd.

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Synthesis of tritium and carbon-14 label
Synthesis of tritium and carbon-14 labelled NNC 61-4655: a potent dual-acting PPARα and PPARγ agonist
✍ Steen K. Johansen; Lars Martiny 📂 Article 📅 2003 🏛 John Wiley and Sons 🌐 French ⚖ 119 KB

## Abstract The synthesis of the potent dual‐acting PPARα and PPARγ agonist NNC 61‐4655 labelled with tritium and carbon‐14 is reported. Tritium labelled NNC 61‐4655 was obtained in three steps with introduction of tritium through catalytic tritium‐halogen exchange of an aryl bromide precursor. Thi