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

被引：3
|
作者：
Fujinaga, Masayuki [1 ]
Ohkubo, Takayuki [1 ]
Yamasaki, Tomoteru [1 ]
Kumata, Katsushi [1 ]
Nengaki, Nobuki [1 ]
Zhang, Ming-Rong [1 ]
机构：
[1] Natl Inst Quantum Sci & Technol, Inst Quantum Med Sci, Dept Adv Nucl Med Sci, Chiba, Chiba 2638555, Japan
来源：
ORGANIC LETTERS | 2022年 / 24卷 / 22期
关键词：
EFFICIENT METHOD; AUTOMATED SYNTHESIS; AROMATIC-AMINES; EPOXIDES; ALCOHOLS; RADIOSYNTHESIS; REACTIVITY; CLEAVAGE; CHLORIDE; LIGANDS;
D O I：
10.1021/acs.orglett.2c01459
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
The scandium triflate-catalyzed N-[F-18]fluoroalkylation of aryl- or heteroaryl-amines with [F-18]epifluorohydrin ([F-18]2) was investigated. This reaction is mild and provides one-step access to N-[F-18]fluor oalkylated 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)-[F-18]2 produced the corresponding enantiomeric N-[F-18]fluoroalkylated anilines.
引用
收藏
页码：4024 / 4028
页数：5
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