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

页码：4024 / 4028

页数：5

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