Anticoagulant compound, composition and application thereof
A compound and composition technology, applied in the field of new coumarin derivatives, can solve the problems of fast dissociation speed, unsatisfactory bioavailability, short half-life and the like
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Embodiment 1
[0078] 1, the preparation of 4-phenyl-3-buten-2-one (7)
[0079]
[0080] Benzaldehyde(6) SCR, AR, d=1.044 106.12 30.5ml 0.3mol 1 acetone SCR, AR, d=0.791 58.08 88ml 1.2mol 4 sodium hydroxide SCR, AR 40 120g 3mol 10 water distilled water 1.08L
[0081] Dissolve 120g of sodium hydroxide in 1.08L of distilled water to make a 10% aqueous solution of sodium hydroxide, cool in an ice bath to 5°C, add 30.5ml of benzaldehyde and 88ml of acetone, stir for 4 hours at 5~10°C, and perform thin-layer chromatography Shows complete reaction. The reaction solution was extracted three times with dichloromethane, and the organic layers were combined, washed with saturated aqueous ammonium chloride until neutral, and dried over anhydrous sodium sulfate overnight. After filtration, the filtrate was concentrated under reduced pressure to obtain a yellow oil. The crude product was distilled under reduced pressur...
Embodiment 2
[0087] SD rats were randomly divided into groups, 10 in each group, half male and half male. A negative control group was set up. Warfarin sodium was used as the positive control drug. 37 hours before the experiment, the drug was given by intragastric administration, the tail of the rat was cut off to collect blood, and the coagulation time was measured.
[0088] Test drug is dissolved in 0.5% CMC solution, and the consumption of embodiment 1 gained compound (2) is 1mg / kg, 3mg / kg, 10mg / kg, 30mg / kg, 100mg / kg; Positive control drug dosage is 1mg / kg. kg, 3mg / kg, 10mg / kg, 30mg / kg, the intragastric volume is 10ml / kg, single intragastric administration. The negative control group was given an equal volume of solvent.
[0089] The coagulation time was used as an index, and the t test was carried out to compare the significance of the difference between the groups.
[0090] See Table 1 for the rat coagulation time results of compound (2) obtained in the example.
[0091] The resu...
Embodiment 3
[0100] SD rats were randomly divided into groups, 4 in each group, half male and half male. A negative control group was set up. Warfarin sodium was used as the positive control drug. 37 hours before the experiment, the drug was given by intragastric administration, the tail of the rat was cut off to collect blood, and the coagulation time was measured.
[0101] The test drug was dissolved in 0.5% CMC solution, the compound (2) obtained in Example 1 and the positive control drug were both used in doses of 10 mg / kg, and the intragastric volume was 10 ml / kg for single intragastric administration. The negative control group was given an equal volume of solvent.
[0102] The coagulation time was used as an index, and the t test was carried out to compare the significance of the difference between the groups.
[0103] The results of coagulation time of test drugs in rats are shown in Table 3.
[0104] Table 3 Experimental results of tail-docking coagulation time in rats
[010...
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