Direct and Regioselective Monofluorination of N-Protected Pyridone Derivatives using N-Fluorobenzenesulfonimide (NFSI)

被引：16

作者：

Sakurai, Fumie ^{[1
]}

Yukawa, Takafumi ^{[1
]}

Taniguchi, Takahiko ^{[1
]}

机构：

[1] Takeda Pharmaceut Co Ltd, Neurosci Drug Discovery Unit, Drug Discovery Chem Labs, 26-1 Muraoka Higashi 2-Chome, Fujisawa, Kanagawa 2518555, Japan

来源：

ORGANIC LETTERS | 2019年 / 21卷 / 18期

关键词：

FLUORINATING AGENTS; DISCOVERY; INHIBITORS; SALTS; TRIFLUOROMETHYLTHIOLATION; CONSTRUCTION; REACTIVITY; RECEPTOR;

D O I：

10.1021/acs.orglett.9b02482

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

The direct monofluorination of N-protected pyridone derivatives has been developed using a stable electrophilic fluorinating reagent, N-fluorobenzenesulfonimide (NFSI). Interestingly, the fluorine atom is regioselectively introduced at the position opposite the carbonyl group in the pyridone substrate during the reaction. This method is applicable to a wide range of substrates and allows the regioselective late-stage monofluorination of pyridone scaffolds.

引用

页码：7254 / 7257

页数：4

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