Antithrombotic compounds as well as preparation methods and applications of antithrombotic compounds
A technology of antithrombotic drugs and compounds, applied in the field of medicine, can solve problems such as high bleeding risk
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Embodiment 1
[0021] .
[0022] Reaction raw materials: self-made, conventional method.
[0023] 1.06 g (10 mmol) of compound II and 1.16 g (10 mmol) of compound III were dissolved in 20 mL of glacial acetic acid and heated to reflux overnight. After the reaction mixture was slightly cooled, it was poured into 200 mL of ice water, stirred, and the solid was collected by suction filtration, recrystallized from absolute ethanol, and vacuum-dried at room temperature to obtain product IV as white crystals. MS, m / z = 205 ([M+H]+).
[0024] 1.02 g (5 mmol) of compound IV, 1.85 g (5 mmol) of compound V and 2.07 g (15 mmol) of solid potassium carbonate were stirred overnight in 15 mL of acetonitrile, and then heated to reflux for 3 hours.
[0025] The reaction mixture was cooled slightly and poured into 200 mL ice water, stirred, adjusted to pH = 4 with concentrated hydrochloric acid, extracted with 50 mL × 3 dichloromethane, combined organic phases, washed with brine, dried over anhydrous sodi...
Embodiment 2
[0026] Example 2 In vitro platelet aggregation inhibition test
[0027] sample Inhibition of Platelet Aggregation IC50 (nM) Compound I 2.7
[0028] It can be seen from the above table that compound I of the present invention exhibits obvious inhibitory effect on platelet aggregation.
Embodiment 3
[0030] Dosage / tablet
[0031] Compound I 10 mg
[0032] Microcrystalline Cellulose 80 mg
[0033] Pregelatinized starch 70 mg
[0034] Polyvinylpyrrolidone 6 mg
[0035] Carboxymethyl starch sodium salt 5 mg
[0036] Magnesium stearate 2 mg
[0037] Talc 2 mg.
[0038] Sieve the active ingredient, pregelatinized starch and microcrystalline cellulose, mix well, add polyvinylpyrrolidone solution, mix, make soft material, sieve, make wet granules, dry at 50-60°C, carboxymethyl Sodium starch salt, magnesium stearate and talc powder are pre-screened and then added to the above granules for tableting.
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