A kind of par-1 antagonist and use thereof
A compound and pharmaceutical technology, applied in the field of drugs related to thrombosis, can solve problems such as high bleeding risk
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Embodiment 1
[0020]
[0021] Reaction raw materials: self-made, conventional method.
[0022] 1.92 g (10 mmol) compound II , 3.70 g (10 mmol) compound III and 4.15 g (30 mmol) of solid potassium carbonate were stirred overnight in 20 mL of acetonitrile, and then heated to reflux for 3 hours.
[0023] 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 sodium sulfate, and dried on a rotary evaporator The solvent was evaporated, and the obtained residue was purified by column chromatography to obtain pure I , white solid, MS, m / z = 518 ([M+Na] + ).
Embodiment 2
[0024] Example 2 In vitro platelet aggregation inhibition test
[0025] sample Inhibitory IC of platelet aggregation 50 (nM) Compound I 1.9
[0026] It can be seen from the above table that the compound of the present invention exhibits obvious inhibitory effect in the platelet aggregation test.
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