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Synthesis of the NK3 receptor antagonist AZD2624 in C-14-, H-3- and C-13-labeled forms

✍ Scribed by Charles S. Elmore; Peter N. Dorff; Mark E. Powell; James E. Hall; Thomas R. Simpson

Publisher: John Wiley and Sons
Year: 2011
Tongue: French
Weight: 222 KB
Volume: 54
Category: Article
ISSN: 0022-2135
DOI: 10.1002/jlcr.1858

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✦ Synopsis

In support of a program to develop an antipsychotic treatment for schizophrenia, three labeled forms of the NK3 receptor antagonist AZD2624 have been prepared. [ 3 H 2 ]AZD2624 was synthesized by tritiodehalogenation for use in receptor occupancy and autoradiographic studies. [ 13 C 6 ]AZD2624 was prepared for use as an internal standard through the intermediacy of [ 13 C 6 ]isatin, and two C-14 isotopomers of AZD2624 were prepared from [ 14 C]benzoic acid and [ 14 C]isatin for a variety of DMPK studies.

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