1029654-30-5Relevant articles and documents
Preparation method of 2-fluoro-4-methyl-3-pyridinylboronic acid
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Paragraph 0010; 0016-0027, (2018/06/15)
The invention belongs to the technical field of organic synthesis, and particularly relates to a preparation method of 2-fluoro-4-methyl-3-pyridinylboronic acid. The preparation method comprises the following steps: performing a lithium-halogen exchange reaction and a boronizing reaction on 2-fluoro-3-bromo-4-methylpyridine serving as a raw material, a lithiation agent and a boronizing agent at alow temperature through a one-pot method to obtain 2-fluoro-4-methyl-3-pyridine ester borate; dehydrating the prepared 2-fluoro-4-methyl-3-pyridine ester borate with a 10 percent by mass sodium hydroxide aqueous solution to obtain a 2-fluoro-4-methyl-3-pyridinylboronic acid crude product; purifying the 2-fluoro-4-methyl-3-pyridinylboronic acid crude product to obtain a 2-fluoro-4-methyl-3-pyridinylboronic acid pure product. In the reaction, tetrahydrofuran is taken as a reaction solvent. The preparation method of the 2-fluoro-4-methyl-3-pyridinylboronic acid has the advantages of low cost, adoption of readily-available raw materials, mild reaction conditions, simple post-treatment operation, lower production cost, high yield, lower reaction cost, and suitability for industrial production.