588677-34-3Relevant academic research and scientific papers
Improved synthesis method for hydrochloric acid acotiamide
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Paragraph 0028, (2019/04/26)
The invention relates to an improved synthesis method for hydrochloric acid acotiamide, and belongs to the field of pharmaceutical chemistry. A cheap compound 1 of 2,4,5-trimethoxybenzoic acid servesas a raw material and is esterfied to obtain an intermediate 2, the intermediate 2 reacts with hydrazine hydrate to generate an intermediate 3, under the acid catalysis, the intermediate 3 reacts withammonium thiocyanate to prepare an intermediate 4, the intermediate 4 reacts with 3-bromine-2-oxopropanoate or 2-chlorine-3-oxopropanoate to generate an intermediate 5 through cyclization, the intermediate 5 and N,N-diisopropyl ethylenediamine are subjected to one-pot ester ammonolysis and demethylation reactions to generate acotiamide, and hydrochloric acid acotiamide 6 is prepared through acidification of concentrated hydrocoloric acid. The adopted raw material is cheap and easy to get, a reaction solvent can be recycled, aftertreatment operation is convenient, the yield and purity are high, particularly, hypertoxic chloride agents and expensive condensing agents are omitted, the ester ammonolysis and demethylation relations are further carried out in one step, the synthesis path is simplified, the cost is reduced, and large-scale industrial production is facilitated. The structure of hydrochloric acid acotiamide is shown in the description.
