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Synthesis of [4-11C]amino acids via ring-opening of aziridine-2-carboxylates

✍ Scribed by N. M. Gillings; A. D. Gee

Publisher
John Wiley and Sons
Year
2001
Tongue
French
Weight
144 KB
Volume
44
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

Ring‐opening of N‐(tert‐butoxycarbonyl)aziridine‐2‐isopropyl carboxylate with no‐carrier‐added (n.c.a.) [^11^C]cyanide is reported. Following purification by HPLC, the protected D,L‐[4‐^11^C]β‐cyanoalanine was subsequently hydrolysed, to yield D,L‐[4‐^11^C]asparagine or D,L‐[4‐^11^C]aspartic acid, or reduced followed by hydrolysis to give D,L‐2,4‐diamino[4‐^11^C]butyric acid. Typical syntheses starting with 10 GBq hydrogen [^11^C]cyanide yielded 1–1.4 GBq of [4‐^11^C]amino acid within 30 min, giving the labelled amino acids in 30–40% decay corrected radiochemical yield (counted from [^11^C]cyanide) with radiochemical purities of 95%, 98% and 60%, respectively. Copyright © 2001 John Wiley & Sons, Ltd.

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