✦ LIBER ✦
Synthesis of a 14C-labeled FPTase inhibitor via a Pd-catalyzed cyanation with Zn(14CN)2 and via bromo[14C]acetic acid
✍ Scribed by Jonathan Z. Ho; Charles S. Elmore; Matthew P. Braun
- Publisher
- John Wiley and Sons
- Year
- 2008
- Tongue
- French
- Weight
- 127 KB
- Volume
- 51
- Category
- Article
- ISSN
- 0022-2135
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✦ Synopsis
Abstract
^14^C‐Labeled farnesyl‐protein transferase inhibitor 1a was required for drug metabolism studies. The first approach was to synthesize ^14^C‐labeled 1b using Zn(^14^CN)~2~ in a Pd‐catalyzed cyanation. A second approach was to prepare labeled 1c with the ^14^C‐label in the piperazine ring. All metabolites from 1b were non‐radioactive whereas the same metabolites from 1c were all radioactive and quantifiable. Copyright © 2008 John Wiley & Sons, Ltd.