- Preparation method of nizatidine bulk drug
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The invention discloses a preparation method of a nizatidine bulk drug. The preparation method comprises the following steps: (1) preparing 2-(N,N-dimethylamino)-4-chloromethyl-4-hydroxy-4,5-dihydrothiazole (III); (2) preparing 2-(N,N-dimethylamino)-4-thiazolemethanol (IV); (3) preparing 2-(dimethylaminomethyl)-4-(2-aminoethylthiomethyl) thiazole (V); and (4) preparing nizatidine. The preparation method has the beneficial effects that the cost is low, the preparation process is simple, the yield is high, and the prepared nizatidine is high in purity.
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Paragraph 0041; 0051; 0060; 0061
(2017/08/25)
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- AN IMPROVED PROCESS FOR PREPARING NIZATIDINE INTERMEDIATE
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The present invention comprises: preparation of dimethylaminothioacetamide by a novel process and its conversion to pure 4-chloromethyl-4-hydroxy-2-dimethylaminomethyl-2-thiazoline by an improved process. The 4-chloromethyl-4-hydroxy-2-dimethylaminomethyl-2-thiazoline obtained by the present invention is substantially of good purity, capable of being used to product commercial quantities of Nizatidine pharmaceutical grade. Dimethylaminothioacetamide is prepared by reacting dimethylaminoacetonitrile with phosphorus pentasulfide, which is then reacted with 1,3-dichloroacetone in dialkylethers, to get substantially pure 4-chloromethyl-4-hydroxy-2-dimethylaminomethyl-2-thiazoline.
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