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

✍ Scribed by Elisabeth Greiner; Arthur J. Atkinson; Alejandro Ayala; George P. Chrousos; Carlo Contoreggi; William C. Eckelman; Philip W. Gold; Kamal E. Habib; Arthur E. Jacobson; Noel Whittaker; Elizabeth L. Webster; Kenner C. Rice

Publisher
John Wiley and Sons
Year
2002
Tongue
French
Weight
103 KB
Volume
45
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

Antalarmin (butyl‐ethyl‐[2,5,6‐trimethyl‐7‐(2,4,6‐trimethyl‐phenyl)‐7__H__‐pyrrolo[2,3‐d]pyrimidin‐4‐yl]‐amine) was doubly labelled with carbon‐13. The synthesized butyl‐[^13^C~2~]ethyl‐[2,5,6‐trimethyl‐7‐(2,4,6‐trimethyl‐phenyl)‐7__H__‐pyrrolo[2,3‐d]pyrimidin‐4‐yl]‐amine (1) and butyl‐ethyl‐[2‐^13^C]‐[2,5,6‐trimethyl‐7‐(2,4,6‐trimethyl‐phenyl)‐7__H__‐pyrrolo[2,3‐d]‐[2‐^13^C] 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% ^13^C). Copyright © 2002 John Wiley & Sons, Ltd.

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