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Dr. Zhanghua Gao, Dr. Yee Hwee Lim, Dr. Matthew Tredwell, Dr. Lei Li, Stefan Verhoog, Dr. Matthew Hopkinson, Wojciech Kaluza, Dr. Thomas Lee Collier, Dr. Jan Passchier, Dr. Mickael Huiban and Prof. Véronique Gouverneur Metal-Free Oxidative Fluorination of Phenols with [18F]Fluoride Angewandte Chemie International Edition 51

Version of Record online: 25 MAY 2012 | DOI: 10.1002/anie.201201502

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The radiochemical synthesis of [18F]4-fluorophenols is based on phenol umpolung under oxidative conditions and direct nucleophilic fluorination with [18F]fluoride (see scheme, TBAF=tetra-n-butylammonium fluoride, TFA=trifluoroacetic acid). Readily available O-unprotected 4-tert-butyl phenols are used as precursors in this one-pot protocol. The reaction is completed in less than 30 minutes at room temperature and can be performed using standard or microfluidic technology.

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