Abstract
The reaction of pyridines with trifluoroacetylated acetylenes was investigated. It was found that the reaction of various pyridines with two molecules of CF3CO-acetylenes proceeds under mild metal-free conditions. As a result, efficient stereoselective synthesis of 3-arylethynyl-3-trifluoromethyl-1,3-oxazinopyridines was elaborated. Target heterocycles can be prepared in up to quantitative yields.
Highlights
Pyridine motif is the one of the most recognizable frameworks among heterocyclic molecules.A lot of attention has been paid to the chemistry of this class of heterocyclic compounds since the very beginning of its discovery
The high attractiveness of pyridine chemistry can be explained by high biological activity of pyridine derivatives both naturally occurred and prepared in the lab
Trifluoromethyl-1,3-oxazinopyridines 3 is presented by the reaction of CF3-ynones withThis pyridines work in
Summary
Pyridine motif is the one of the most recognizable frameworks among heterocyclic molecules.A lot of attention has been paid to the chemistry of this class of heterocyclic compounds since the very beginning of its discovery. Pyridine motif is the one of the most recognizable frameworks among heterocyclic molecules. The high attractiveness of pyridine chemistry can be explained by high biological activity of pyridine derivatives both naturally occurred and prepared in the lab. Almost 300 alkaloids, having pyridine moiety (not including derivatives with fused pyridine ring, such as isoquinoline), were listed in “The Dictionary of Alkaloids” [1]. The pyridine scaffold is a privileged structure for design of novel pharmaceuticals. Structural analysis of US FDA approved drugs showed that pyridine core is a consistent part of 62 marketed drugs (second place after piperidine) in the list of most frequent nitrogen heterocycles in structure of approved drugs [2,3]. One can found 15 derivatives of pyridine among the “Top 200 Pharmaceutical
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