Synthesis of deuterated BCX-34 (peldesine)

Article abstract of DOI:10.1002/(SICI)1099-1344(19991230)42:13<1235::AID-JLCR279>3.0.CO;2-Q

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.