Trifluoroacetyl-HYNIC peptides: Synthesis and Tc-99m radiolabeling

Surfraz, M. Bashir-Uddin and King, Robert C. and Mather, Stephen J. and Biagini, Stefano C. G. and Blower, Philip J. (2007) Trifluoroacetyl-HYNIC peptides: Synthesis and Tc-99m radiolabeling. Journal of Medicinal Chemistry, 50 (6). pp. 1418-1422. ISSN 0022-2623 . (The full text of this publication is not currently available from this repository. You may be able to access a copy if URLs are provided)

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Official URL
http://dx.doi.org/10.1021/jm061274l

Abstract

Fmoc-lys(HYNIC-Boc)-OH, a precursor for solid-phase synthesis of Tc-99m-labeled peptides, was synthesized efficiently without HPLC purification. HPLC-ESMS showed that deprotection and decoupling of peptide from the resin with trifluoroacetic acid gave initially HYNIC-peptide, which was trifluoroacetylated upon prolonged incubation. The trifluoroacetyl-HYNIC group was hydrolyzed during Tc-99m labeling, rendering deprotection unnecessary. Trifluoroacetyl-HYNIC peptide was Tc-99m-labeled as efficiently, producing the same product, as HYNIC-peptide. These modifications enhance the versatility of HYNIC for Tc-99m peptide labeling.

Item Type: Article
Subjects: Q Science > QD Chemistry
Divisions: Faculties > Science Technology and Medical Studies > School of Biosciences
Faculties > Science Technology and Medical Studies > School of Physical Sciences > Functional Materials Group
Faculties > Science Technology and Medical Studies > School of Physical Sciences
Depositing User: Jane Griffiths
Date Deposited: 14 May 2008 07:04
Last Modified: 12 May 2014 08:55
Resource URI: https://kar.kent.ac.uk/id/eprint/3105 (The current URI for this page, for reference purposes)
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