简单快捷地获得新型氟化噻唑并[3,2-a]嘧啶-7-酮和噁唑并[3,2-a]嘧啶-7-酮衍生物及其通过钯催化反应的功能化。
Simple and Expedient Access to Novel Fluorinated Thiazolo- and Oxazolo[3,2-]pyrimidin-7-one Derivatives and Their Functionalization via Palladium-Catalyzed Reactions.
机构信息
Laboratoire de Physico-Chimie des Matériaux et des Electrolytes pour l'Energie (PCM2E), EA 6299, Avenue Monge, Faculté des Sciences, Université de Tours, Parc de Grandmont, 37200 Tours, France.
Laboratoire des Composés Hétéro-Organiques et Matériaux Nanostructurés (LR18ES11), Faculté des Sciences de Bizerte, Université de Carthage, Zarzouna 7021, Tunisie.
出版信息
Molecules. 2022 May 7;27(9):3013. doi: 10.3390/molecules27093013.
An efficient, versatile, and one-pot method for the preparation of novel fluorinated thiazolo- and oxazolo[3,2-]pyrimidin-7-ones is described from 2-aminothiazoles or 2-amino-oxazoles and fluorinated alkynoates. This transformation, performed under transition-metal-free conditions, offers new fluorinated cyclized products with good to excellent yields. Moreover, the functionalization of these -fused scaffolds via the Suzuki-Miyaura and Sonogashira cross-coupling reactions led to the synthesis of highly diverse thiazolo- and oxazolo[3,2-]pyrimidin-7-ones.
本文描述了一种高效、通用且一锅法制备新型氟化噻唑并[3,2-a]嘧啶-7-酮和氧化噻唑并[3,2-a]嘧啶-7-酮的方法，该方法由 2-氨基噻唑或 2-氨基恶唑与氟化炔酸酯反应得到。此转化在无过渡金属条件下进行，可得到具有良好至优异收率的新型氟化环化产物。此外，通过 Suzuki-Miyaura 和 Sonogashira 交叉偶联反应对这些稠合骨架进行官能化，可合成高度多样化的噻唑并[3,2-a]嘧啶-7-酮和氧化噻唑并[3,2-a]嘧啶-7-酮。
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