Efficient Syntheses of Dual Radioisotope-Labelled PF-00217830, a D2-Partial Agonist for the Treatment of Schizophrenia Disorder-Reference-Cited by-同舟云学术

Efficient Syntheses of Dual Radioisotope-Labelled PF-00217830, a D2-Partial Agonist for the Treatment of Schizophrenia Disorder

Published:2012-06 Issue:6 Volume:36 Page:351-355
ISSN:1747-5198
Container-title:Journal of Chemical Research
language:en
Short-container-title:Journal of Chemical Research

Author:

Zhang Yinsheng¹,Garnes Keith T.²,Brown Donna³

Affiliation:

1. Radiochemistry Group, Chemical RandD, Groton Labs, Pfizer Inc. Groton, C T, USA

2. Synthesis Services, Radiosynthesis, ABC Laboratories Inc. Columbia, MO, USA

3. Donna Brown Consulting, Groton, CT, USA

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.

Publisher

SAGE Publications

Subject

General Chemistry

Link

http://journals.sagepub.com/doi/pdf/10.3184/174751912X13359587895460

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