110925-92-3Relevant academic research and scientific papers
A preparation method for rosacea acetate hydrochloride
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, (2021/12/07)
The present invention relates to the field of pharmaceutical preparation technology, in particular to a method for preparing rosatidine acetate hydrochloride. The present invention adopts m-hydroxybenzoic acid as a starting material, a wide range of sources, inexpensive, and it can be prepared by oxidation of m-hydroxytoluene, without involving a toxicity warning structure and nitrosamine impurities; at the same time, in this preparation process only involves a genotoxic warning structure substance, reducing the risk of medication of subsequent drugs.
Novel preparation method of intermediate namely 3-(1-piperidine methyl)phenol of roxatidine acetate hydrochloride
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Paragraph 0070-0073, (2018/04/02)
The invention relates to a preparation method of an intermediate namely 3-(1-piperidine methyl)phenol of roxatidine acetate hydrochloride. M-nitrobenzaldehyde is taken as the primary raw material; under the effect of a phase transfer catalyst, m- nitrobenzaldehyde is reduced by metal borohydride to obtain corresponding benzyl alcohol; in the presence of an alkali, benzyl alcohol reacts with organic sulfonyl chloride to generate active organic sulfonate; then in the presence of an alkali, organic sulfonate carries out N-alkylation reactions with piperidine to generate N-substituted piperidine derivatives; reducing the nitro groups of N-substituted piperidine derivatives to obtain corresponding amino compounds; and subjecting the amino compounds to diazotization, hydrolysis, and alkalizationin a sulfuric acid water solution to obtain 3-(1-piperidine methyl)phenol. The problem that the supply of the conventional raw material (m-hydroxyl benzaldehyde) is not enough and the cost is greatlyincreased is solved. The method is simple and safe, the raw materials are cheap and easily available, the reaction yield is high, and the method is very suitable for industrial production of 3-(1-piperidine methyl)phenol.
