Potent and selective CC chemokine receptor 1 antagonists labeled with carbon-13, carbon-14, and tritium

J Labelled Comp Radiopharm. 2018 May 15. doi: 10.1002/jlcr.3635. Online ahead of print.

Abstract

1-(4-Fluorophenyl)-1H-pyrazolo[3,4-c]pyridine-4-carboxylic acid (2-methanesulfonyl-pyridin-4-ylmethyl)-amide (1) and its analogs (2) and (3) are potent CCR1 antagonists intended for the treatment of rheumatoid arthritis. The detailed syntheses of these 3 compounds labeled with carbon-13 as well as the preparation of (1) and (2) labeled with carbon-14, and (1) labeled with tritium, are described.

Keywords: CCR1 antagonists; carbon-13; carbon-14; radiosynthesis; tritium.