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Synthesis of 14 C‐ and 2 H‐labelled CHF6001: A new potent PDE4 inhibitor
Author(s) -
Fontana E.,
Cenacchi V.,
Pivetti F.,
Pignatti A.,
Pazzi T.,
Bondanza L.,
Pazzi M.
Publication year - 2017
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.3537
Subject(s) - chemistry , yield (engineering) , radiochemistry , cyanide , carbon 14 , chemical synthesis , nuclear chemistry , stereochemistry , organic chemistry , biochemistry , in vitro , materials science , metallurgy , physics , quantum mechanics
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.