Synthesis of doubly 13C‐labelled antalarmin isotopomers for pharmacokinetic studies

Antalarmin (butyl‐ethyl‐2,5,6‐trimethyl‐7‐(2,4,6‐trimethyl‐phenyl)‐7H‐pyrrolo2,3‐d]pyrimidin‐4‐yl]‐amine) was doubly labelled with carbon‐13. The synthesized butyl‐¹³C₂]ethyl‐2,5,6‐trimethyl‐7‐(2,4,6‐trimethyl‐phenyl)‐7H‐pyrrolo2,3‐d]pyrimidin‐4‐yl]‐amine ( 1 ) and butyl‐ethyl‐2‐¹³C]‐2,5,6‐trimethyl‐7‐(2,4,6‐trimethyl‐phenyl)‐7H‐pyrrolo2,3‐d]‐2‐¹³C] pyrimidin‐4‐yl]‐amine, ( 2 ) were prepared for use as substrates for pharmacokinetic studies. These compounds were obtained in fair overall yield in a 5 and 6 step synthesis (20–24.5%, respectively) and high isotopic purity (about 99 at% ¹³C). Copyright © 2002 John Wiley & Sons, Ltd.