Abstract
PF-00217830 is a D2-partial agonist developed for the treatment of schizophrenia. The dual 14C/14C and 14C/3H-labelled PF-00217830 were required for animal and human absorption, distribution, metabolism and elimination (ADME) studies. This report describes the development of the syntheses of dual 14C/14C- and dual 14C/3H-labelled PF-00217830. [14C]PF-00217830-L labelled at the naphthalene ring was prepared in three steps starting with [14C]naphthalene, while [3H]PF-00217830-R was synthesised by Pd-catalysed tritium de-bromination of brominated PF-00217830 in a single radiosynthetic step. The dual [14C/3H]PF-00217830 was made by mixing 1:10 radioactivity ratio of [14C]PF-00217830-L and [3H]PF-00217830-R. The chemistry for [14C]PF-00217830-R labelled at the pyridine ring was also described.
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