New Directions In C-H Fluorination

New Directions In C-H Fluorination



One-step transformations from C–H to C–F are attractive methods especially if fluorine can be introduced at a late-stage of the synthesis. However, C–H fluorination is still an unsolved problem with just few successful approaches so far (as opposed to all other halogenation reactions). In this opinion, we highlight the challenges associated with C–H fluorination and discuss current …


8/1/2019  · Traditional C–H fluorination reactions were developed with highly active reagents (e.g.


F 2, hypofluorites, or electrochemical methods), but such reactions have so far not been amenable for the synthesis of functionally complex molecules due to the harsh reaction conditions 15.


16..The development of novel fluorinating reagents (e.g.


diethylaminosulfur trifluoride and Selectfluor) have …


New Directions in C–H Fluorination Qiang Cheng1 and Tobias Ritter1,* One-step transformations from C–HtoC–F are attractive methods especially if ?uorine can be introduced at a late-stage of the synthesis. However, C–H ?uorination is still an unsolved problem with just few successful approaches so, Download Citation | New Directions in C–H Fluorination | One-step transformations from C–H to C–F are attractive methods especially if fluorine can be introduced at a late-stage of the …


New Directions in C–H Fluorination . By Q. Cheng and T. Ritter. Cite . BibTex Full citation Abstract. One-step transformations from C–H to C–F are attractive methods especially if fluorine can be introduced at a late-stage of the synthesis. However, C–H fluorination is still an unsolved problem with just few successful approaches so …


However, C–H fluorination is still an unsolved problem with just few successful approaches so far (as opposed to all other halogenation reactions). In this opinion, we highlight the challenges associated with C–H fluorination and discuss current progress for three different classes: directed fluorination , aliphatic fluorination , and …


Recent advances in C–H functionalization have allowed new approaches to C–F bonds. Herein we highlight progress in C–H fluorination, which is arguably the most efficient approach to incorporate fluorine since it obviates the need of pre-functionalization of organic compounds.


Site-selective fluorination of aliphatic C–H bonds remains synthetically challenging. While directed C–H fluorination represents the most promising approach, the limited work conducted to date has enabled just a few functional groups as the arbiters of direction. Leveraging insights gained from both computat, Late-stage C–H fluorination is an appealing reaction for medicinal chemistry. However, the application of this strategy to process research appears less attractive due to the formation and necessary purification of mixtures of organofluorines. Here we demonstrate that ?-fluoroleucine methyl ester, an intermediate critical to the large-scale synthesis of odanacatib, can be accessed directly …


Qiang Cheng, Tobias Ritter, New Directions in C–H Fluorination, Trends in Chemistry, 10.1016/j.trechm.2019.04.001, (2019). Crossref Kelley E. Danahy, Julian C. Cooper, Jeffrey F. Van Humbeck, Benzylic Fluorination of Aza?Heterocycles Induced by Single?Electron Transfer to Selectfluor, Angewandte Chemie International Edition, 10.1002/anie.201801280, 57 , 18, (5134-5138), (2018).

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