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1-[18F]fluoro-2-propanol p-toluenesulfonate: a synthon for the preparation of N-([18F]fluoroisopropyl)amines
Affiliation:1. High Institute of Nursing and Health Techniques of Rabat, Ministry of Health, Rabat, Morocco;2. Laboratory of Plant Chemistry and Organic and Bioorganic Synthesis, URAC23, Faculty of Science, GEOPAC, Mohammed V University in Rabat, Morocco;3. Cátedra de Química General, Instituto de Química Inorgánica, Facultad de Bioquímica, Química y Farmacia, Universidad Nacional de Tucumán, Ayacucho 471, Tucumán 4000, Argentina;4. Sorgun Vocational School, Science and Art Faculty-Department of Physics, Yozgat Bozok University, Yozgat, Turkey;5. Department of Physics, Faculty of Artsand Sciences, Ondokuz Mayıs University, Samsun, Turkey;6. Chemical & Biochemical Sciences Green-Process Engineering (CBS-GPE), Mohammed VI Polytechnic University, Lot 660, Hay Moulay Rachid, Benguerir, Morocco;7. Laboratory of Analytical Chemistry and Bromatology, Team of Formulation and Quality Control of Health Products, Faculty of Medicine and Pharmacy, Mohammed V University in Rabat, Morocco;1. Jiangsu Key Laboratory of Micro and Nano Heat Fluid Flow Technology and Energy Application, Suzhou University of Science and Technology, Suzhou 215009, China;2. School of Physical Science and Technology, Suzhou University of Science and Technology, Suzhou 215009, China;3. Key Laboratory of Low-grade Energy Utilization Technologies and Systems (Chongqing University), Ministry of Education of China, Chongqing University, Chongqing 400044, China;4. College of Engineering and Technology, Southwest University, Chongqing 400715, China;5. School of Chemistry and Life Sciences, Suzhou University of Science and Technology, Suzhou 215009, China;1. Division of Nephrology, Guangdong General Hospital, Guangdong Academy of Medical Sciences, Guangzhou, China;2. Southern Medical University, Guangzhou, China;1. Centre de Recherche en Cancérologie Nantes-Angers, INSERM, U892, Equipe Apoptose et Progression Tumorale, 8 Quai Moncousu, BP7021, 44007 Nantes, France;2. Université de Nantes, Faculté de Médecine, Département de Recherche en Cancérologie, IFR26, F-44000 Nantes, France;3. Institut de Cancérologie de l''Ouest – LaBCT, René Gauducheau, Boulevard J. Monod, F-44805 St Herblain, France;4. Laboratory for Epigenetics and Environnement, Centre National de Génotypage, CEA – Institut de Génomique, F-91000 Evry, France;5. Membre du réseau Epigénétique du Cancéropole Grand Ouest, France
Abstract:The new radiochemical synthon 1-[18F]fluoro-2-propanol p-toluenesulfonate 2′a is prepared with a radiochemical yield of 45% [corrected for decay to beginning of synthesis (BOS), synthesis time 40 min]. This compound is used to prepare the [18F]fluoroisopropyl-alkylated derivatives of benzylamine and norephedrine with a yield of 7 and 2% respectively (BOS, synthesis time 90 min). This alkylation reaction with 2′a gives a good perspective for the preparation of [18F]fluoro-labelled analogues of β1-adrenergic receptor binding ligands for PET.
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