Stereospecific radiosynthesis of 3-fluoro amino acids: access to enantiomerically pure radioligands for positron emission tomography.

Org Biomol Chem

Realomics Strategic Research Initiative, Department of Chemistry, University of Oslo, Sem salands vei 26, 0374, Oslo, Norway. and Norsk Medisinsk Syklotron AS, Nydalen, Oslo, Norway and Klinikk for Kirugi og Nevrofag, Oslo Universitet Sykehus HF-Rikshopitalet, Nydalen, Oslo, Norway.

Published: March 2018

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Article Abstract

A variety of substituted non-racemic aziridine-2-carboxylates equivalent to amino acids were prepared and subjected to ring opening reaction by [18F/19F]fluoride. The regio and stereospecific ring opening depends on the substituents on the nitrogen as well as both the carbons of aziridines. The applicability of the methods to afford access to 3-[18F/19F]fluoro amino acids are illustrated.

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http://dx.doi.org/10.1039/C8OB00184GDOI Listing

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