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

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Direct and Regioselective Monofluorination of N-Protected Pyridone Derivatives using N-Fluorobenzenesulfonimide (NFSI)
Organic Letters ( IF 4.9 ) Pub Date : 2019-09-06 , DOI: 10.1021/acs.orglett.9b02482
Fumie Sakurai ₁ , Takafumi Yukawa ₁ , Takahiko Taniguchi ₁

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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.

中文翻译：

使用N-氟苯磺酰亚胺（NFSI）对N保护的吡啶酮衍生物进行直接和区域选择性单氟化

已使用稳定的亲电氟化试剂N-氟苯磺酰亚胺（NFSI）开发了N-保护的吡啶酮衍生物的直接单氟化。有趣的是，在反应过程中，氟原子在与吡啶酮底物中的羰基相反的位置上区域选择性地引入。该方法适用于广泛的底物，并允许吡啶酮支架的区域选择性晚期单氟化。

更新日期：2019-09-06

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