Selective [N-15(2)eta] labelling of an N-G-propionylated arginine derivative

Kleinmaier, Roland and Gschwind, Ruth M. (2009) Selective [N-15(2)eta] labelling of an N-G-propionylated arginine derivative. JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 52 (1-2). pp. 29-32. ISSN 0362-4803,

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Abstract

A straightforward convergent synthesis of [N-15(2)eta]-Bz-Arg(N-eta-propionyl)-OEt*TFA is presented. In this approach, the guanidinylation reagent [N-15(2)]-N(boc)-N'(propionyl)-S-methylisothiourea is reacted with the side chain amino group of the title compound's ornithine precursor. The guanidinylation step is promoted by stoichiometric addition of HgCl2 to force completion. This method leads directly to the N-G-acylated product and the acyl residue is principally modifiable in the last synthetic step of the guanidinylation reagent.

Item Type: Article
Uncontrolled Keywords: PROTECTED GUANIDINES; AMINES; GUANYLATION; REAGENTS; DESIGN; N-15-labelling; arginine; S-methylisothiourea
Subjects: 500 Science > 540 Chemistry & allied sciences
Divisions: Chemistry and Pharmacy > Institut für Organische Chemie > Arbeitskreis Prof. Dr. Ruth Gschwind
Depositing User: Dr. Gernot Deinzer
Date Deposited: 12 Oct 2020 13:09
Last Modified: 12 Oct 2020 13:09
URI: https://pred.uni-regensburg.de/id/eprint/29772

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