Monohydrate crystal of fimasartan potassium salt, its preparation method and pharmaceutical composition containing it
A technology of fimasartan and monohydrate, which is applied in the direction of drug combinations, organic chemical methods, and medical preparations containing active ingredients, can solve the problems of increased processing costs, troubles, economic losses, etc., and achieve the goal of reducing processing time Effect
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Embodiment 1
[0115] Embodiment 1: Preparation of Fimasartan potassium salt monohydrate
[0116] By adding 2-n-butyl-5-dimethylaminothiocarbonylmethyl-6-methyl-3-[[2'-(1H-tetrazol-5-yl) to isopropanol (18.5 mL) Biphenyl-4-yl]methyl]pyrimidin-4(3H)-one (hereinafter referred to as Fimasartan) (6.55 g, 12.6 mmol) was used to prepare a suspension.
[0117] To the prepared suspension was added a solution prepared by mixing isopropanol (19.6 mL), potassium hydroxide (1.18 g, 21.0 mmol) and 2-ethylhexanoic acid (2.83 g, 19.6 mmol), dissolved at 81°C , then stirred at reflux for 1 hour. Then, the mixture was cooled to 25°C to precipitate crystals, and the obtained solid was filtered and washed successively with isopropanol (2.5 mL) and ethyl acetate (2.0 mL).
[0118] Then, the crystals were dried at 40° C. for 8 hours under a reduced pressure of 10 mmHg to yield fimasartan potassium salt monohydrate in the form of a white powder solid.
[0119] Yield: 6.49g (95.5%)
[0120] Moisture content (KF ...
Embodiment 2
[0121] Embodiment 2: Preparation of Fimasartan potassium salt monohydrate
[0122] A suspension was prepared by adding Fimasartan (8.52 g, 16.4 mmol) to isopropanol (18.5 mL).
[0123] To the prepared suspension was added a solution prepared by mixing isopropanol (19.6 mL), potassium hydroxide (1.18 g, 21.0 mmol) and 2-ethylhexanoic acid (2.83 g, 19.6 mmol), dissolved at 81°C , then stirred at reflux for 1 hour. Then, the mixture was cooled to 25°C to precipitate crystals, and the obtained solid was filtered and washed with isopropanol (2.5 mL) and ethyl acetate (2.0 mL).
[0124] Then, the crystals were dried at 40° C. for 8 hours under a reduced pressure of 10 mmHg to yield fimasartan potassium salt monohydrate in the form of a white powder solid.
[0125] Yield: 8.35g (94.4%)
[0126] Moisture content (KF method): 3.70%
Embodiment 3
[0127] Embodiment 3: Preparation of Fimasartan potassium salt monohydrate
[0128] A suspension was prepared by adding Fimasartan (8.91 g, 17.1 mmol) to isopropanol (18.5 mL).
[0129] To the prepared suspension was added a solution prepared by mixing isopropanol (19.6 mL), potassium hydroxide (1.18 g, 21.0 mmol) and 2-ethylhexanoic acid (2.83 g, 19.6 mmol), dissolved at 81°C , then stirred at reflux for 1 hour. Then, the mixture was cooled to 25°C to precipitate crystals, and the obtained solid was filtered and washed with isopropanol (2.5 mL) and ethyl acetate (2.0 mL).
[0130] Then, the crystals were dried at 40° C. for 8 hours under a reduced pressure of 10 mmHg to yield fimasartan potassium salt monohydrate in the form of a white powder solid.
[0131] Yield: 8.65g (93.8%)
[0132] Moisture content (KF method): 3.44%
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