56026-52-9Relevant articles and documents
Preparation method of nicotinic acid derivative
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Paragraph 0060-0061, (2019/12/02)
The invention relates to a preparation method of a nicotinic acid derivative. The method comprises the following steps: with N-benzylpiperidine-4-keto-3-formate as a raw material, carrying out a hydrogenolysis reaction to obtain piperidine-4-keto-3-formate; performing halogenation reaction with a certain amount of a halogenation reagent to obtain 3,5-dihalogenated piperidine-4-one-3-formate or 3,5,5-trihalogenated piperidine-4-one-3-formateperforming one-pot process with different alkaline reagent for removing halogen hydride through elimination, and performing hydrolysis and performing acidification with hydrochloric to generate corresponding nicotinic acid derivatives: 4-hydroxynicotinic acid, 4-aminonicotinic acid, 4-hydroxy-5-chloronicotinic acid, 4-amino-5-chloronicotinic acid and 4-amino-5-bromonicotinic acid. The method is simple and convenient to operate, mild in condition, short in technological process, low in wastewater amount, environmentally friendly and low in cost, and green industrial production of the nicotinic acid derivative is facilitated.
