846033-37-2Relevant articles and documents
Efficient syntheses of dual radioisotope-labelled PF-00217830, a D 2-partial agonist for the treatment of schizophrenia disorder
Zhang, Yinsheng,Garnes, Keith T.,Brown, Donna
, p. 351 - 355 (2012/09/21)
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.
7-(4-(4-[3-CHLORO-2-(TRIFLUOROMETHYL)PHENYL]PIPERAZIN-1-YL)BUTOXY)-[1,8]-NAPHTHYRIDIN-2(1H)-ONE
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Page/Page column 7, (2008/12/06)
This invention relates to a compound of formula (I) or pharmaceutically acceptable salts thereof, pharmaceutical compositions containing the compound or a salt thereof, and its use as a medicament for the treatment of schizophrenia, bipolar disorder, or other central nervous system disorders.