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Carbon-11 labelled analogs of alanine by the strecker synthesis

✍ Scribed by Christian Prenant; Annemarie Theobald; Thilo Siegel; Jürgen Joachim; Klaus Weber; Uwe Haberkorn; Franz Oberdorfer

Publisher
John Wiley and Sons
Year
1995
Tongue
French
Weight
373 KB
Volume
36
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

Derivatives of alanine, α‐[2‐^11^C]aminoisobutyric acid 1a and α‐(N‐methyl)‐[2‐^11^C]aminoisobutyric acid 1b were prepared for the in‐vivo study of amino acid transport phenomena by positron‐emission‐tomography (PET). Compounds 1a and 1b were obtained by a Zelinski‐Stadnikoff variant of the Strecker α‐amino acid synthesis from in‐situ formed [^11^C]acetone in presence of sodium cyanide and either ammonium sulfate (for 1a) or methylamine hydrochloride (for 1b). The complete preparation required 50 min from the end of [^11^C]CO~2~ production, and delivered 1.2 ‐ 2 GBq of labelled product for application (2.4 ‐ 4%; not corrected for decay; related to trapped [^11^C]CO~2~). The specific activity of the labelled products was 16 to 20 GBq·μmol^−1^. The radiochemical and chemical purity of the preparations was greater than 98%.

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