Convenient Entry to 18 F-Labeled Amines through the Staudinger Reduction

Autor:	Matthias M. Herth, Christoph Denk, E. Johanna L. Stéen, Vladimir Shalgunov, Andreas Kjaer, Hannes Mikula, Jesper L. Kristensen
Rok vydání:	2019
Předmět:	Reduction (complexity) Primary (chemistry) 010405 organic chemistry Chemistry Bioactive molecules Organic Chemistry Synthon Physical and Theoretical Chemistry Pet tracer 010402 general chemistry 01 natural sciences Combinatorial chemistry 0104 chemical sciences
Zdroj:	European Journal of Organic Chemistry. 2019:1722-1725
ISSN:	1434-193X
DOI:	10.1002/ejoc.201801457
Popis:	Fluorine-18 possesses outstanding decay characteristics for positron emission tomography (PET) imaging. Therefore, it is ideally suited for clinical applications. As such, improved strategies to incorporate fluorine-18 into bioactive molecules are of utmost importance. Indirect 18F-labeling with amino-functionalized synthons is a convenient and versatile approach to synthesize a broad variety of PET tracers. Herein, we report a method to convert 18F-labeled azides to primary amines by means of the Staudinger reduction. Aliphatic and aromatic 18F-labeled azides were converted into the corresponding amines with high conversion yields. The method was easily automated. From a broader perspective, the applied strategy results in two useful synthons from a single precursor and thus increases the flexibility to label diverse chemical scaffolds with minimal synthetic effort.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::f610694acda0761e8ace03a849e98bae https://doi.org/10.1002/ejoc.201801457 Zobrazit plný text záznamu Plný text ve formátu PDF Plný text ve formátu HTML
Nepřihlášeným uživatelům se plný text nezobrazuje	K zobrazení výsledku je třeba se přihlásit.