A5080865905- Radiopharmaceutical Chemistry and Applications
- Medical Imaging Techniques and Applications
- Fluorine in Organic Chemistry
- Chemical Synthesis and Analysis
- Catalytic C–H Functionalization Methods
- Neuroscience and Neuropharmacology Research
- Alzheimer's disease research and treatments
- Catalytic Cross-Coupling Reactions
- Lung Cancer Treatments and Mutations
- Dendrimers and Hyperbranched Polymers
- Trace Elements in Health
- Mass Spectrometry Techniques and Applications
- Click Chemistry and Applications
- Cholinesterase and Neurodegenerative Diseases
- Chemical Reactions and Isotopes
- Synthesis and Catalytic Reactions
- Synthetic Organic Chemistry Methods
- Cyclopropane Reaction Mechanisms
Massachusetts General Hospital
2014-2020
Harvard University
2013-2020
Centre for Addiction and Mental Health
2019-2020
University of the West Indies System
2019-2020
University of Toronto
2019
Gordon Center for Medical Imaging
2015-2016
University of Wisconsin–Madison
2009-2015
Imaging Center
2015
Madison Group (United States)
2014
The carbon−nitrogen bond of carboxamides is extremely stable under most conditions. present study reveals that simple zirconium− and hafnium−amido complexes are highly efficient catalysts for equilibrium-controlled transamidation reactions between secondary amines tertiary amides. In a number cases, proceeds rapidly at room temperature. We find these new sufficiently active to promote the metathesis amides, which arises from successive cycles. catalytic activities we observe unprecedented...
New chemistry methods for the synthesis of radiolabeled small molecules have potential to impact clinical positron emission tomography (PET) imaging, if they can be successfully translated. However, progression modern reactions from stage synthetic development preparation radiotracer doses ready use in human PET imaging is challenging and rare. Here we describe process successful translation a palladium-mediated fluorination reaction non-human primate (NHP) baboon imaging-an important...
Translation of new methodologies for labeling nonactivated aromatic molecules with <sup>18</sup>F remains a challenge. Here, we report one-step, regioselective, metal-free <sup>18</sup>F-labeling method that uses hypervalent iodonium(III) ylide precursor, to prepare the radiopharmaceutical <sup>18</sup>F-3-fluoro-5-[(pyridin-3-yl)ethynyl]benzonitrile (<sup>18</sup>F-FPEB). <b>Methods:</b> Automated radiosynthesis <sup>18</sup>F-FPEB was achieved by reaction precursor (4 mg)...
Abstract Lorlatinib (PF-06463922) is a next-generation small-molecule inhibitor of the orphan receptor tyrosine kinase c-ros oncogene 1 (ROS1), which has domain that physiologically related to anaplastic lymphoma (ALK), and undergoing Phase I/II clinical trial investigations for non-small cell lung cancers. An early goal measure concentrations this drug in brain tumour lesions cancer patients, as penetration blood–brain barrier important optimal therapeutic outcomes. Here we prepare both 11...
A metal-free and selective method to form [<sup>18</sup>F]aryl-CF<sub>2</sub>H through nucleophilic radiofluorination of benzyl (pseudo)halides oxidative C–H activation benzylic bonds has been developed.
Fluorine-18 labeled 2-fluoro-8-hydroxyquinoline ([(18)F]CABS13) is a promising positron emission tomography (PET) radiopharmaceutical based on metal chelator developed to probe the "metal hypothesis of Alzheimer's disease". Herein, practical radiosynthesis [(18)F]CABS13 was achieved by radiofluorination followed deprotection an O-benzyloxymethyl group. Automated production and formulation resulted in 19 ± 5% uncorrected radiochemical yield, relative starting [(18)F]fluoride, with ≥95%...
[18F]FPEB is a positron emission tomography (PET) radiopharmaceutical used for imaging the abundance and distribution of mGluR5 in central nervous system (CNS). Efficient radiolabeling aromatic ring has been an ongoing challenge. Herein, five metal-free precursors radiofluorination were compared, namely, chloro-, nitro-, sulfonium salt, two spirocyclic iodonium ylide (SCIDY) bearing cyclopentyl (SPI5) new adamantyl (SPIAd) auxiliary. The chloro- nitro-precursors resulted low radiochemical...
Anilides undergo phosphoric acid-promoted ammonolysis to primary amides in a diol solvent, such as ethylene glycol.
There is a great demand to develop more cost‐efficient and robust manufacturing processes for fluorine‐18 ( 18 F) labelled compounds radiopharmaceuticals. Herein, we present our knowledge the first radiofluorination “in‐loop,” where [ F]triflyl fluoride was used as labelling agent. Initial development of “in‐loop” F]fluorination method optimized by reacting with 1,4‐dinitrobenzene form F]1‐fluoro‐4‐nitrobenzene. This methodology then applied syntheses two well‐known radiopharmaceuticals,...