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J Labelled Comp Radiopharm ; 60(12): 577-585, 2017 10.
Article in English | MEDLINE | ID: mdl-28763109

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.


Subject(s)
Carbon Radioisotopes/chemistry , Cyclic Nucleotide Phosphodiesterases, Type 4/metabolism , Deuterium/chemistry , Phosphodiesterase 4 Inhibitors/chemistry , Phosphodiesterase 4 Inhibitors/chemical synthesis , Sulfonamides/chemistry , Sulfonamides/chemical synthesis , para-Aminobenzoates/chemistry , para-Aminobenzoates/chemical synthesis , Chemistry Techniques, Synthetic , Isotope Labeling , Phosphodiesterase 4 Inhibitors/pharmacology , Sulfonamides/pharmacology , para-Aminobenzoates/pharmacology
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