Deoxyfluorination of phenols.
نویسندگان
چکیده
An operationally simple ipso fluorination of phenols with a new deoxyfluorination reagent is presented.
منابع مشابه
18F-Deoxyfluorination of Phenols via Ru π-Complexes
The deficiency of robust and practical methods for 18F-radiofluorination is a bottleneck for positron emission tomography (PET) tracer development. Here, we report the first transition-metal-assisted 18F-deoxyfluorination of phenols. The transformation benefits from readily available phenols as starting materials, tolerance of moisture and ambient atmosphere, large substrate scope, and translat...
متن کاملDeoxyfluorination of alcohols with 3,3-difluoro-1,2-diarylcyclopropenes
Aromatic cation activation is a useful strategy to promote deoxyfunctionalization; however, the deoxyfluorination of alcohols with cyclopropenium cation remains an unsolved problem due to the weak nucleophilicity of fluoride ion. Here we report the use of 3,3-difluoro-1,2-diarylcyclopropenes (CpFluors) as easily accessible and reactivity-tunable deoxyfluorination reagents. The electronic nature...
متن کاملHDAC6 Brain Mapping with [18F]Bavarostat Enabled by a Ru-Mediated Deoxyfluorination
Histone deacetylase 6 (HDAC6) function and dysregulation have been implicated in the etiology of certain cancers and more recently in central nervous system (CNS) disorders including Rett syndrome, Alzheimer's and Parkinson's diseases, and major depressive disorder. HDAC6-selective inhibitors have therapeutic potential, but in the CNS drug space the development of highly brain penetrant HDAC in...
متن کاملPhenoFluor: Practical Synthesis, New Formulation, and Deoxyfluorination of Heteroaromatics
We report a practical synthesis method of the reagent PhenoFluor on decagram scale, provide a new formulation of PhenoFluor as a toluene solution, which should decrease challenges associated with the moisture sensitivity of the reagent, and expand the substrate scope of deoxyfluorination with PhenoFluor to heteroaromatics.
متن کاملThe first synthesis and cytostatic activity of novel 6-(fluoromethyl)purine bases and nucleosides.
Two alternative approaches to the synthesis of novel 6-(fluoromethyl)purine bases and nucleosides are described either by direct deoxyfluorination or by multistep functional group transformations starting from 6-(hydroxymethyl)purines. 6-(fluoromethyl)purine ribonucleoside displayed significant cytostatic effects.
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
عنوان ژورنال:
- Journal of the American Chemical Society
دوره 133 30 شماره
صفحات -
تاریخ انتشار 2011