Scandium Triflate-Catalyzed N -[ 18 F]Fluoroalkylation of Aryl- Or Heteroaryl-Amines with [ 18 F]Epifluorohydrin under Mild Conditions.

Autor: Fujinaga M; Department of Advanced Nuclear Medicine Sciences, Institute for Quantum Medical Science, National Institutes for Quantum Science and Technology, 4-9-1 Anagawa, Inage-ku, Chiba, Chiba 263-8555, Japan., Ohkubo T; Department of Advanced Nuclear Medicine Sciences, Institute for Quantum Medical Science, National Institutes for Quantum Science and Technology, 4-9-1 Anagawa, Inage-ku, Chiba, Chiba 263-8555, Japan.; SHI Accelerator Service Ltd., 1-17-6 Osaki, Shinagawa-ku, Tokyo 141-0032, Japan., Yamasaki T; Department of Advanced Nuclear Medicine Sciences, Institute for Quantum Medical Science, National Institutes for Quantum Science and Technology, 4-9-1 Anagawa, Inage-ku, Chiba, Chiba 263-8555, Japan., Kumata K; Department of Advanced Nuclear Medicine Sciences, Institute for Quantum Medical Science, National Institutes for Quantum Science and Technology, 4-9-1 Anagawa, Inage-ku, Chiba, Chiba 263-8555, Japan., Nengaki N; Department of Advanced Nuclear Medicine Sciences, Institute for Quantum Medical Science, National Institutes for Quantum Science and Technology, 4-9-1 Anagawa, Inage-ku, Chiba, Chiba 263-8555, Japan.; SHI Accelerator Service Ltd., 1-17-6 Osaki, Shinagawa-ku, Tokyo 141-0032, Japan., Zhang MR; Department of Advanced Nuclear Medicine Sciences, Institute for Quantum Medical Science, National Institutes for Quantum Science and Technology, 4-9-1 Anagawa, Inage-ku, Chiba, Chiba 263-8555, Japan.
Jazyk: angličtina
Zdroj: Organic letters [Org Lett] 2022 Jun 10; Vol. 24 (22), pp. 4024-4028. Date of Electronic Publication: 2022 May 25.
DOI: 10.1021/acs.orglett.2c01459
Abstrakt: The scandium triflate-catalyzed N -[ 18 F]fluoroalkylation of aryl- or heteroaryl-amines with [ 18 F]epifluorohydrin ([ 18 F] 2 ) was investigated. This reaction is mild and provides one-step access to N -[ 18 F]fluoroalkylated aryl- or heteroaryl-amines, which are used for positron emission tomography imaging. The use of 2,2,2-trifluoroethanol as a cosolvent improved the reaction efficiency. The use of ( S )- and ( R )-[ 18 F] 2 produced the corresponding enantiomeric N -[ 18 F]fluoroalkylated anilines.
Databáze: MEDLINE
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