Convergent synthesis of ¹³N-labelled Peptidic structures using aqueous [¹³N]NH₃.

ABSTRACT:

Background

Nitrogen-13 has a 10-min half-life which places time constraints on the complexity of viable synthetic methods for its incorporation into PET imaging agents. In exploring ways to overcome this limitation, we have used the Ugi reaction to develop a rapid one-pot method for radiolabelling peptidic molecules using [¹³N]NH₃ as a synthetic precursor.

Methods

Carrier-added [¹³N]NH₃ (50 μL) was added to a solution of carboxylic acid, aldehyde, and isocyanide in 2,2,2-TFE (200 μL). The mixture was heated in a microwave synthesiser at 120 °C for 10 min. Reactions were analysed by radio-HPLC and radio-LCMS. Isolation of the target ¹³N-labelled peptidic Ugi compound was achieved via semi-preparative radio-HPLC as demonst

SUBMITTER: Blower JE 

PROVIDER: S-EPMC5824707 | biostudies-literature | 2017

REPOSITORIES: biostudies-literature