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Dr. Qianghui Zhou, Alessandro Ruffoni, Ryan Gianatassio, Dr. Yuta Fujiwara, Dr. Eran Sella, Prof. Dr. Doron Shabat and Prof. Dr. Phil S. Baran Direct Synthesis of Fluorinated Heteroarylether Bioisosteres Angewandte Chemie International Edition 52

Version of Record online: 4 MAR 2013 | DOI: 10.1002/anie.201300763

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(Bioiso)steering in a new direction: A modular synthesis of reagents (e.g. sodium difluoroethylsulfinate) that can be used for the direct incorporation of difluoroalkyl groups onto heterocycles is reported. The scope and generality of the incorporation of difluoroalkyl groups is exemplified with the difluoroethyl group and a proof of principle is shown for a general synthesis of fluorinated heteroarylether bioisosteres.

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