- Synthetic method of triamterene intermediate
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The invention improves a synthesis method of triamterene from an intermediate to a triamterene finished product. The method adopts guanidine hydrochloride as a starting material to prepare 5-nitroso-2, 4, 6-triaminopyrimidine, and comprises the following steps: (1) sequentially adding water and malononitrile into a reaction kettle, stirring for 25 minutes for dissolving, starting nitrogen protection, adding a sodium nitrite saturated solution at 20 DEG C, dropwise adding 8% HCl at the same time for adjusting the pH value to 3-4, after the sodium nitrite aqueous solution is dropwise added, keeping the temperature for 2.5 hours at 18 DEG C, wherein the dosage weight ratio of the water to the sodium nitrite to the malononitrile to the 8% hydrochloric acid is as follows: the use mass ratio of the sodium nitrite to the malononitrile to the 8% hydrochloric acid is 2.5:1.15:1:0.35; and (2) adding guanidine hydrochloride solid into the solution obtained in the step (1), and stirring for 30 minutes, and adding NaCO3 solid to adjust the pH value to 9-10, wherein the weight ratio of guanidine hydrochloride to sodium carbonate to malononitrile in (1) is as follows: guanidine hydrochloride to malononitrile to sodium carbonate is 1.60:1:(0.10-0.12). According to the method, the synthesis risk of the triamterene intermediate is reduced, wastewater generated in the refining process is reduced, and safe production, energy conservation and emission reduction are facilitated.
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Paragraph 0015-0017
(2021/07/28)
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- Triamterene compound and preparation method thereof
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The invention relates to a triamterene compound and a preparation method thereof. The triamterene compound is a crystal. The triamterene compound prepared by the method provided by the invention has high purity and good stability, and the preparation method of triamterene has the characteristics of simplicity, stable product quality, and small environmental pollution, and is suitable for further promotion and application.
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Paragraph 0011; 0013; 0015
(2018/04/02)
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- A preparation method of the pteridine phenalgin (by machine translation)
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The invention relates to a preparation method of the pteridine phenalgin, comprises the following steps: adding to the condensation reaction kettle 5 - nitroso - 2, 4, 6 - triaminopyrimidine and benzyl cyanide, adding non-proton polar solvent under stirring condition by adding alkaline catalyst, heating to 50 - 120 °C insulation 3 - 10 h after cooling to 0 - 50 °C, filtering to obtain phenalgin pteridine crude product, crude adopts the non-proton polar solvent refining, washing to obtain the final product phenalgin pteridine. The invention using a suitable solvent as reaction and refining solvent, can make the reaction yield 85.7%, effectively reduce the production cost, and reduce the pollutants such as; using a suitable solvent refining, can effectively reduce the refined solvent consumption, improve the purification efficiency, refining solvent can be recycled by distilling and then mechanically, no waste water is produced, environmental pollution is small, the material can be recycled, the purity of the product and the like, suitable for further popularization and application. (by machine translation)
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Paragraph 0022-0039
(2017/08/29)
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- Potassium-neutral salureticum with anti-hypertensive effect
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A diuretically active combination comprising furosemide and triamterene in a ratio of 1:1 to 1:2, in which furosemide is in the form of controlled release so as to facilitate solubilization of the furosemide in triamterene micelles to stabilize the combination as mixed micelles of low polydispersity yielding dissolution rates in in vitro tests of furosemide of not more than about 1.5% after about one hour at pH 1.5 to 3.5 and a slow release of not more than about 4.5% at pH 5.5 concurrent with a release of triamterene of about 60-70% and 80%, respectively, and with a release of not more than 85% furosemide after eight hours at pH 7.5 in salt solutions of adjusted pH.
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