185104-11-4Relevant articles and documents
Preparation method of acotiamide hydrochloride impurity
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Paragraph 0022; 0024, (2020/08/02)
The invention discloses a preparation method of an acotiamide hydrochloride impurity. The method comprises the following steps: carrying out acylating chlorination on a raw material 2,4,5-trimethoxybenzoic acid to obtain 2,4,5-trimethoxybenzoyl chloride, and carrying out an amidation reaction on the 2,4,5-trimethoxybenzoyl chloride and 2-amino-4-ethoxycarbonyl-1,3-thiazole to obtain 2-amino-4-ethoxycarbonyl-1,3-thiazole (intermediate 1); hydrolyzing the intermediate 1 with sodium hydroxide to obtain 2-[N-(2,4,5-trimethoxybenzoyl)amino]-4-carboxyl-1,3-thiazole (intermediate 2); and performing an acylating chlorination reaction on the intermediate 2 to obtain an acyl chloride group, performing an amidation reaction on the acyl chloride group and N,N-diisopropylethylenediamine to obtain N-[2-(diisopropylamino)ethyl]-2-[(2,4,5-trimethoxybenzoyl)amino]-4-thiazole formamide (acotiamide), and performing a salt forming reaction on the acotiamide to obtain acotiamide hydrochloride. The preparation method of the acotiamide hydrochloride impurity has the advantages of mild reaction conditions, simple operation, low cost and high yield, and is suitable for industrial production.
IMPROVED METHOD FOR MANUFACTURING ACOTIAMIDE
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Paragraph 0029, (2019/06/20)
PROBLEM TO BE SOLVED: To provide a method for manufacturing acotiamide or acotiamide hydrochloride trihydrate capable of avoiding the use of 2,4,5-trimethoxy benzoyl chloride that is an intermediate manufactured by using thionyl chloride. SOLUTION: There is provided a method for manufacturing acotiamide or acotiamide hydrochloride trihydrate comprising the steps of: manufacturing 2-[(2,4,5-trimethoxy benzoyl) amino]-1,3-thiazole-4-ethyl carboxylate from 2,4,5-trimethoxy benzoic acid S- (benzothiazole-2-yl) and 2-amino-1,3-thiazole-4-ethyl carboxylate; manufacturing 2-[(2-hydroxy-4,5-dimethoxy benzoyl) amino]-1,3-thiazole-4-ethyl carboxylate by demethylation; and reacting the resultant product with N,N-diisopropyl ethylenediamine to manufacture acotiamide. SELECTED DRAWING: None COPYRIGHT: (C)2019,JPOandINPIT
A synthesis method of arab League tests for the amine hydrochloride
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, (2017/08/25)
The invention relates to a synthetic method of acotiamide hydrochloride. The synthetic route of the acotiamide hydrochloride comprises the following steps: protecting hydroxyl vicinal to carboxyl in a formula (1) compound to obtain a formula (2) compound,