Synthesis of deuterated-BCX-34 (peldesine)

Abstract

BCX-34 (peldesine) is a novel purine nucleoside phosphorylase inhibitor that is in human clinical trials for the treatment of T-cell cancers and for HIV infected patients. In support of our BCX-34 clinical program, a mass spectrometric assay has been developed utilizing a deuterated-BCX-34 analog as an internal standard. The synthesis of tetra-deuterated-BCX-34 (peldesine) from ethyl nicotinate (2,4,5,6-[2H]4) is described in this report. Copyright © 1999 John Wiley & Sons, Ltd.