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

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

Journal of labelled compounds & radiopharmaceuticals (2018-05-17)
Bachir Latli, Matt Hrapchak, Maxim Cheveliakov, Jonathan T Reeves, Maurice Marsini, Carl A Busacca, Chris H Senanayake
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.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
6-Chloro-3-pyridinecarbonitrile, 97%