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. 2017 Oct;60(12):577-585.
doi: 10.1002/jlcr.3537. Epub 2017 Sep 18.

Synthesis of 14 C- and 2 H-labelled CHF6001: A new potent PDE4 inhibitor

E Fontana  1 , V Cenacchi  2 , F Pivetti  3 , A Pignatti  1 , T Pazzi  4 , L Bondanza  4 , M Pazzi  4
Affiliations

Synthesis of 14 C- and 2 H-labelled CHF6001: A new potent PDE4 inhibitor

E Fontana et al. J Labelled Comp Radiopharm. 2017 Oct.

Abstract

An 8-step preparation of 14 C-labelled CHF6001, a potent phosphodiesterase 4 inhibitor in the treatment of respiratory diseases, is described. An overall yield of approximately 9% was obtained starting from copper[14 C]cyanide. The synthesis of a stable labelled version of CHF6001 is also reported using the commercially available trideuterated bromomethylcyclopropane as starting material.

Keywords: CHF6001; PDE4 inhibitor; carbon-14; deuterium; internal standard.

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