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

In support of a program to develop an antipsychotic treatment for schizophrenia, three labeled forms of the NK3 receptor antagonist AZD2624 have been prepared. [3H2]AZD2624 was synthesized by tritiodehalogenation for use in receptor occupancy and autoradiographic studies. [13C6]AZD2624 was prepared for use as an internal standard through the intermediacy of [13C6]isatin, and two C-14 isotopomers of AZD2624 were prepared from [14C]benzoic acid and [14C]isatin for a variety of DMPK studies. Copyright © 2011 John Wiley & Sons, Ltd.