Synthesis of tritium labelled delta sleep-inducing peptide

✍ Scribed by Matthieu Giraud; Jean-Louis Morgat; Florine Cavelier; Jean Martinez

• Publisher: John Wiley and Sons
• Year: 2001
• Tongue: French
• Weight: 110 KB
• Volume: 44
• Category: Article
• ISSN: 0022-2135
• DOI: 10.1002/jlcr.477

✦ Synopsis

Abstract

The α,β‐dehydro precursor of the delta sleep‐inducing peptide (DSIP) for tritiation was prepared prior to tritiation using a 3+6 fragment coupling strategy on a solid support. The first fragment, α,β‐dehydrotripeptide, was prepared in solution in five steps in 79% overall yield while the second fragment was obtained by a step by step peptide synthesis on a Wang resin using an Fmoc strategy. The α,β‐dehydrotripeptide was coupled to the fragment linked to the resin, followed by a deprotection/cleavage step to yield the α,β‐dehydro‐DSIP, 7. Catalytic reduction of unsaturated DSIP using tritium gas and palladium oxide as catalyst gave [^3^H]DSIP having a specific activity of 1.184 TBq/mmol(32 Ci/mmol). Copyright © 2001 John Wiley & Sons, Ltd.