Pyridine derivative compound and preparation method thereof

Abstract

The invention discloses a pyridine derivative compound and a preparation method thereof. The preparation method comprises the steps: in an inert gas atmosphere, sequentially adding heterocyclic quaternary phosphonium salt, iodide, alkali, a silver additive, a palladium catalyst and a phosphorus ligand into a solvent, to obtain a mixture, wherein the molar ratio of the heterocyclic quaternary phosphonium salt to the iodide to the alkali to the silver additive to the palladium catalyst to the phosphorus ligand is (2.5-25):(1-10):(3-30):(1.2-12):(0.5-5):(1-10), and the molar volume ratio of the iodide to the solvent is 0.1 mmol:1 mL; and then, in an inert gas atmosphere, carrying out reaction on the mixture at the temperature of 62-68 DEG C for 11-13 h, and collecting a reaction product, namely the pyridine derivative compound. According to the preparation method, the adopted raw materials are simple and easy to obtain, the substrate range is wide, the cost is low, the reaction conditionsare mild, and the catalyst dosage is extremely small.

Description

technical field [0001] The invention belongs to the technical field of organic chemical synthesis, and in particular relates to a pyridine derivative compound and a preparation method thereof. Background technique [0002] Pyridine derivative compounds based on nitrogen heterocycles such as pyridine and diazine are important pharmacophores, which widely exist in biologically active compounds, drugs, functional materials and ligands, and have very important practical value. Therefore, both academia and industry have high requirements and strong interest in its synthesis method. At present, there are three main strategies to realize the functionalization of pyridine: [0003] (1) Direct functionalization of nitrogen heterocycles via C–H bond activation is an effective means for selectively introducing different groups. In the method disclosed in Document 1 (Yoshiaki Nakao, Kyalo Stephen Kanyiva, Tamejiro Hiyama. J. Am. Chem. Soc. 2008, 130, 2448-2449), the nitrogen atom of py...

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Problems solved by technology

[0009] However, the above strategies have limitations to varying degrees, including poor reaction selectivity, narrow scope of application, and difficult synthesis of raw materials, making it difficult to apply them in production.

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