Synthesis of [18F]-γ-Fluoro-α,β-unsaturated Esters and Ketones via Vinylogous 18F-Fluorination of α-Diazoacetates with [18F]AgF

Autor: Stephen Thompson, Peter Scott, Melanie S. Sanford, Isaac M. Jackson, Allen F. Brooks, So Jeong Lee, Naoko Ichiishi
Rok vydání: 2019
Předmět:
Zdroj: Synthesis. 51:4401-4407
ISSN: 1437-210X
0039-7881
Popis: This communication reports a method for the vinylogous radiofluorination of α-diazoacetates to generate [18F]-γ-fluoro-α,β-unsaturated esters and ketones in moderate to good radiochemical yields. The method uses no-carrier-added [18F]AgF and is compatible with aromatic and non-aromatic substrates and a number of different functional groups. The labeling method is showcased in the synthesis of a fluorinated cholest-5-en-3-one derivative as well as a difluorinated product pertinent to drug discovery.
Databáze: OpenAIRE