期刊
EUROPEAN JOURNAL OF ORGANIC CHEMISTRY
卷 2019, 期 23, 页码 3751-3762出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/ejoc.201900300
关键词
Deoxyradiofluorination; Aziridinium; Aminoester; Fluorine-18; Radiochemistry
资金
- Region Normandie
- CNRS
- CEA, Labex IRON [ANR-11-LABX-0018-01, FR3038 INC3M]
We report the conversion of beta-hydroxy-alpha-aminoesters derived from serine, alpha-methylserine or beta-phenylserine to the corresponding [F-18]fluorinated alpha or beta-aminoesters by deoxyradiofluorination using [F-18]fluoride. The method involved the ring opening of an aziridinum intermediate formed in situ in the presence of a base after activation of the alcohol function with triflic anhydride. The overall process was carried out at room temperature. Both the efficiency and the regioselectivity of the reaction were found to be dependent on the starting substrates. [F-18]Fluoroaminoesters were obtained in radiochemical yields ranging from 10-75 %. No improvement was observed for reactions carried out under heating.
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