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ChemicalBook CAS DataBase List Triamterene

Triamterene synthesis

2synthesis methods
Triamterene, 2,4,7-triamino-6-phenylpteridine (21.5.13), is synthesized in by the following scheme. Reacting guanidine with malonodinitrile gives 2,4,6-triaminopyrimidine (21.5.11). This undergoes nitrosation by reacting it with nitric acid, which results in the formation of 5-nitroso-2,4,6-triaminopyrimidine (21.5.12), which upon condensation with benzyl cyanide in the presence of sodium methoxide cyclizes into triamterene (21.5.13).

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Yield:396-01-0 85.7%

Reaction Conditions:

with sodium ethanolate;sodium hydroxide in ethanol;N,N-dimethyl acetamide at 90 - 100;Reagent/catalyst;

Steps:

1 The method of producing the triamterene, Characterized in that the preparation method comprises the following steps:
To the reaction kettle into the 400kg reaction with DMAC, 100kg 5-nitroso-2,4,6-triaminopyrimidine,120kgPhenylacetonitrile,5kg solid sodium hydroxide, stir, at 20-30 ° C, start dropping37kgEthanol sodium ethanol solution,1-2h drops finished, after the drop slowly heated to 90-100 ° C, 5h after the insulation after cooling to 30 ° C, the material was filtered to remove the crude albendrobin crude. refined The crude dibenzopropenidine crude product into the refining kettle, put 1200kg refined with DMAC, stirring up to 110-120 ° C, filtered while hot, the filtrate into the crystallization kettle, the filtrate cooled to 20-25 ° C, filtered and dried, the ammonia benzene dish 140.8kg, the yield of 85.7%, content of 99.64%

References:

Yancheng Maidike Chemicals To Make Co., Ltd.;Yu Suogeng;Yan Zhengming;Yang Yong CN106967069, 2017, A Location in patent:Paragraph 0022-0039

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