Efficient DBU accelerated synthesis of F-labelled trifluoroacetamides.

Chem Commun (Camb)

AstraZeneca Personalised Healthcare and Biomarkers, PET Centre at Karolinska Institutet, Karolinska Universitetssjukhuset Solna, R5:02, SE-171 76 Stockholm, Sweden. and Stockholm Brain Institute, Karolinska Institutet, SE-171 77 Stockholm, Sweden and Department of Clinical Neuroscience, Karolinska Institutet, S-17176 Stockholm, Sweden.

Published: November 2016

Nucleophilic F-fluorination of bromodifluoromethyl derivatives was performed using [F]BuNF in the presence of DBU (1,8-diazabicyclo[5.4.0]undec-7-ene). This novel procedure provided a diverse set of [F]trifluoroacetamides in good to excellent radiochemical conversions. A mechanism where DBU acts as organomediator in this transformation is proposed.

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Source
http://dx.doi.org/10.1039/c6cc08535kDOI Listing

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