Synthesis of PNU‐159548 labelled with ¹⁴C and ²H

Abstract

The cytotoxic antitumor compound PNU‐159548 (1) has been labelled with 14C and 2H. A three‐step sequence starting from [14‐14C]idarubicin (2a) led to radiochemically pure (>98%) [14‐14C]PNU‐159548 with a specific activity of 1.13 GBq/mmol. The synthesis of [2H4]PNU‐159548 was carried out in a similar manner starting from [1,1,2,2‐2H4]2‐bromoethanol (3b). Copyright © 2002 John Wiley & Sons, Ltd.